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PMID:26445 | Characterization of receptors mediating 5-hydroxytryptamine- and catecholamine-induced platelet aggregation, assessed by the actions of alpha- and beta-blockers, butyrophenones, 5-HT antagonists and chlorpromazine. | 1 Blood platelets from normal human volunteers were isolated and aggregated in vitro with 5-hydroxytryptamine (5-HT), noradrenaline (NA), dopamine and N-dimethyldopamine (DMDA). 2 The effects of 5-HT antagonists, alpha- and beta-adrenoceptor blocking agents, butyrophenones and chlorpromazine upon aggregation induced by... | Characterization of receptors mediating 5-hydroxytryptamine- and catecholamine-induced platelet aggregation, assessed by the actions of alpha- and beta-blockers, butyrophenones, 5-HT antagonists and chlorpromazine. 1 Blood platelets from normal human volunteers were isolated and aggregated in vitro with 5-hydroxytrypta... | [
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PMID:26446 | Biochemical evidence for the dual action of labetalol on alpha- and beta-adrenoceptors. | 1 Labetalol (AH 5158A) inhibited the adrenaline-stimulated adenylate cyclase activity of rat liver and heart. This drug had no effect on basal or guanosine triphosphate (GTP)-activated adenylate cyclase activities. 2 Labetalol displaced the binding of the specific ligands [3H]-dihydroergocryptine and (-)-[3H]-dihydroal... | Biochemical evidence for the dual action of labetalol on alpha- and beta-adrenoceptors. 1 Labetalol (AH 5158A) inhibited the adrenaline-stimulated adenylate cyclase activity of rat liver and heart. This drug had no effect on basal or guanosine triphosphate (GTP)-activated adenylate cyclase activities. 2 Labetalol displ... | [
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PMID:26447 | The treatment of frigidity: a comparative study of group and individual desensitization. | Forty patients took part in this study. Twenty patients treated by group desensitization were compared with twenty treated by individual desensitization. Group desensitization appeared the more effective treatment if outcome was measured on the patients' self-rating scale, but the less effective if outcome was measured... | The treatment of frigidity: a comparative study of group and individual desensitization. Forty patients took part in this study. Twenty patients treated by group desensitization were compared with twenty treated by individual desensitization. Group desensitization appeared the more effective treatment if outcome was me... | [
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PMID:26450 | Antibiotic resistance in Streptococcus pneumoniae and Haemophilus influenzae. Report of a study group on bacterial resistance. | Twenty laboratories in England and Scotland took part in 1977 in a survey of antibiotic resistance in Streptococcus pneumoniae and Haemophilus influenzae. In Str pneumoniae 59 (6.8%) of the 866 strains studied were resistant to tetracycline and three to chloramphenicol, and one strain showed a decreased susceptibility ... | Antibiotic resistance in Streptococcus pneumoniae and Haemophilus influenzae. Report of a study group on bacterial resistance. Twenty laboratories in England and Scotland took part in 1977 in a survey of antibiotic resistance in Streptococcus pneumoniae and Haemophilus influenzae. In Str pneumoniae 59 (6.8%) of the 866... | [
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PMID:26452 | Recurrent genital candidosis in women and the effect of intermittent prophylactic treatment. | A study of clotrimazole for the treatment of recurrent genital candidosis unexpectedly showed that symptoms and infection can be dissociated. The aim of the study was to see if intermittent antifungal treatment would reduce symptoms in women constantly distressed by recurrent genital candidosis. Forty women seriously a... | Recurrent genital candidosis in women and the effect of intermittent prophylactic treatment. A study of clotrimazole for the treatment of recurrent genital candidosis unexpectedly showed that symptoms and infection can be dissociated. The aim of the study was to see if intermittent antifungal treatment would reduce sym... | [
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PMID:26455 | [Nycthemeral plasma and testicular androgen contents in guinea pigs at puberty]. | A study based upon transversal sampling involving 13 series of 7 animals each does not show a significant circadian rhythm of testosterone and delta4 androstenedione concentrations in the plasma and testis of the guinea-pig at the age of puberty. | [Nycthemeral plasma and testicular androgen contents in guinea pigs at puberty]. A study based upon transversal sampling involving 13 series of 7 animals each does not show a significant circadian rhythm of testosterone and delta4 androstenedione concentrations in the plasma and testis of the guinea-pig at the age of p... | [
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PMID:26456 | Energy-driven uptake of humic acids by Aspergillus niger. | The uptake of humic acids by mycelia of Aspergillus niger was demonstrated to be energy-dependent with a sensitivity to sodium azide and to 2,4-dinitrophenol. Greater uptake of humic acids by submerged mycelium occurred at pH 3.0 and at 32 degrees C. The rate of uptake was influenced by the concentration of humic acids... | Energy-driven uptake of humic acids by Aspergillus niger. The uptake of humic acids by mycelia of Aspergillus niger was demonstrated to be energy-dependent with a sensitivity to sodium azide and to 2,4-dinitrophenol. Greater uptake of humic acids by submerged mycelium occurred at pH 3.0 and at 32 degrees C. The rate of... | [
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PMID:26457 | Induction of autolysis in Bacillus subtilis by ochratoxin A. | Ochratoxin A (OTA) added during the exponential growth phase at a concentration higher than 12 microgram/ml caused autolysis of Bacillus subtilis. Optical density of cultures decreased, and at higher concentrations the cultures became sterile. Optimum OTA-induced lysis was about pH 5. At concentrations below 10 microgr... | Induction of autolysis in Bacillus subtilis by ochratoxin A. Ochratoxin A (OTA) added during the exponential growth phase at a concentration higher than 12 microgram/ml caused autolysis of Bacillus subtilis. Optical density of cultures decreased, and at higher concentrations the cultures became sterile. Optimum OTA-ind... | [
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PMID:26458 | Antifungal properties of 2-alkynoic acids and their methyl esters. | Thirteen 2-alkynoic acids and their methyl esters (C3--C12, C14, C16, and C18) were tested against Aspergillus niger, Trichoderma viride, and Myrothecium verrucaria in Sabouraud dextrose agar at pH 4.0 and 5.6. Toxicity to Candida albicans, Trichophyton mentagrophytes, and Mucro mucedo was determined in the same medium... | Antifungal properties of 2-alkynoic acids and their methyl esters. Thirteen 2-alkynoic acids and their methyl esters (C3--C12, C14, C16, and C18) were tested against Aspergillus niger, Trichoderma viride, and Myrothecium verrucaria in Sabouraud dextrose agar at pH 4.0 and 5.6. Toxicity to Candida albicans, Trichophyton... | [
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PMID:26459 | Prescribing of psychoactive drugs for chronically ill elderly patients. | The prescribing of psychoactive drugs for 1431 chronically ill elderly patients being assessed for long-term institutional or community care was surveyed. Psychoactive drugs had been prescribed for about one quarter of the patients; benzodiazepines were the most frequently prescribed group. Judging from the extensive p... | Prescribing of psychoactive drugs for chronically ill elderly patients. The prescribing of psychoactive drugs for 1431 chronically ill elderly patients being assessed for long-term institutional or community care was surveyed. Psychoactive drugs had been prescribed for about one quarter of the patients; benzodiazepines... | [
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PMID:26460 | Clinical pharmacology and therapeutics of benzodiazepines. | Benzodiazepines are among the most commonly prescribed drugs in the world. In contrast to their extensive use, the therapeutic indications and potential of benzodiazepines are limited. All benzodiazepine derivatives available in Canada are similar structurally and in their pharmacologic actions. Few have specific advan... | Clinical pharmacology and therapeutics of benzodiazepines. Benzodiazepines are among the most commonly prescribed drugs in the world. In contrast to their extensive use, the therapeutic indications and potential of benzodiazepines are limited. All benzodiazepine derivatives available in Canada are similar structurally ... | [
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PMID:26462 | Heat fractionation and thermotolerance: a review. | A rational approach to the design of clinical protocols combining fractionated hyperthermia plus X-irradiation or hyperthermia plus chemotherapy requires an understanding of the biology of fractionated heat alone. Mammalian cells growing in vitro can dramatically increase their tolerance to thermal damage (i.e., reduce... | Heat fractionation and thermotolerance: a review. A rational approach to the design of clinical protocols combining fractionated hyperthermia plus X-irradiation or hyperthermia plus chemotherapy requires an understanding of the biology of fractionated heat alone. Mammalian cells growing in vitro can dramatically increa... | [
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PMID:26464 | Purification and properties of acid ribonucleases in human serum and leukocytes. | Acid RNase was purified from normal human serum about 2400-fold by chromatography on phosphocellulose and Sephadex G-75 and rechromatography on Sephadex G-75. Assayed with yeast RNA as substrate, the enzyme showed the maximal activity at about pH 6.5 with sodium phosphate buffer. The reaction was activated by Na+, K+, ... | Purification and properties of acid ribonucleases in human serum and leukocytes. Acid RNase was purified from normal human serum about 2400-fold by chromatography on phosphocellulose and Sephadex G-75 and rechromatography on Sephadex G-75. Assayed with yeast RNA as substrate, the enzyme showed the maximal activity at a... | [
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PMID:26465 | Serum acid ribonuclease in myelogenous leukemia. | Acid and alkaline RNase activities in serum were measured with yeast RNA as the substrate in normal subjects and in leukemic patients pretreatment and posttreatment, and the acid/alkaline ratios of activities were 0.63 +/- 0.08 (S.D.) (N, 12), 2.28 +/- 0.82 (N, 8), and 0.60 +/- 0.13 (N, 9), respectively. The mean value... | Serum acid ribonuclease in myelogenous leukemia. Acid and alkaline RNase activities in serum were measured with yeast RNA as the substrate in normal subjects and in leukemic patients pretreatment and posttreatment, and the acid/alkaline ratios of activities were 0.63 +/- 0.08 (S.D.) (N, 12), 2.28 +/- 0.82 (N, 8), and 0... | [
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PMID:26467 | Changes in small vessel blood content of the rat heart induced by hypercapnic, hyperoxic or asphyxic conditions. | The small vessel blood content (SVBC) of the ventricular walls of the heart of anesthetized closed chest rats was determined using 59FeC13 to label the plasma siderophilin. SVBC was measured breathing air, 100% O2, 5% CO2 in 21% O2 and during asphyxia. The average SVBC could be ranked: air less than 100% O2 less than 5... | Changes in small vessel blood content of the rat heart induced by hypercapnic, hyperoxic or asphyxic conditions. The small vessel blood content (SVBC) of the ventricular walls of the heart of anesthetized closed chest rats was determined using 59FeC13 to label the plasma siderophilin. SVBC was measured breathing air, 1... | [
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PMID:26479 | [Purification of rat brain guanylate cyclase]. | The purification of guanylate cyclase has been achieved. After electrophoresis on polyacrylamide gel only one protein band was observed. The low factor of purification must therefore be ascribed to the loss of an activator of guanylate cyclase. Stimulation of the activity by nitroprusside is also lost during purificati... | [Purification of rat brain guanylate cyclase]. The purification of guanylate cyclase has been achieved. After electrophoresis on polyacrylamide gel only one protein band was observed. The low factor of purification must therefore be ascribed to the loss of an activator of guanylate cyclase. Stimulation of the activity ... | [
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PMID:26481 | Isolation of gamma-glutamyltransferase from human liver, and comparison with the enzyme from human kidney. | We isolated gamma-glutamyltransferase [(gamma-glutamyl)-peptide:amino acid gamma-glutamyltransferase, EC 2.3.2.2] from human liver and compared some of its properties with the same enzyme prepared from human kidney. The enzymes from these two sources are very similar with respect to initial velocity kinetic constants, ... | Isolation of gamma-glutamyltransferase from human liver, and comparison with the enzyme from human kidney. We isolated gamma-glutamyltransferase [(gamma-glutamyl)-peptide:amino acid gamma-glutamyltransferase, EC 2.3.2.2] from human liver and compared some of its properties with the same enzyme prepared from human kidne... | [
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PMID:26483 | Biochemical characterization of an aryl acetic ester hydrolase isolated from human monocytes. | A carboxylic-ester hydrolase was isolated from the leukocytes of a patient with myelomonocytic leukemia. Its relative molecular mass as estimated by sucrose density-gradient sedimentation is about 70 000. The purified enzyme is specific for acetyl esters of aromatic alcohols. It is inhibited by fluoride, but insensitiv... | Biochemical characterization of an aryl acetic ester hydrolase isolated from human monocytes. A carboxylic-ester hydrolase was isolated from the leukocytes of a patient with myelomonocytic leukemia. Its relative molecular mass as estimated by sucrose density-gradient sedimentation is about 70 000. The purified enzyme i... | [
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PMID:26484 | A novel gamma-glutamyl transpeptidase in renal carcinoma in comparison with normal kidney enzyme. | A novel gamma-glutamyl transpeptidase was found in a renal carcinoma tissue. This enzyme electrophoresed more quickly than that of normal kidney, but more slowly than normal liver enzyme. Their Rf values are 0.46, 0.33, and 0.52 for the renal carcinoma, normal kidney and normal liver enzyme, respectively. After treatme... | A novel gamma-glutamyl transpeptidase in renal carcinoma in comparison with normal kidney enzyme. A novel gamma-glutamyl transpeptidase was found in a renal carcinoma tissue. This enzyme electrophoresed more quickly than that of normal kidney, but more slowly than normal liver enzyme. Their Rf values are 0.46, 0.33, an... | [
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PMID:26485 | A simple radioimmunoassay for plasma cortisol. | A simple radioimmunoassay (RIA) for plasma cortisol is described which combines the advantages of (i) direct analysis of untreated plasma samples, (ii) use of solid-coupled anti-cortisol antibodies and (iii) use of a gamma-labelled radioligand. The reagents are relatively easily prepared and stable, and the analysis ca... | A simple radioimmunoassay for plasma cortisol. A simple radioimmunoassay (RIA) for plasma cortisol is described which combines the advantages of (i) direct analysis of untreated plasma samples, (ii) use of solid-coupled anti-cortisol antibodies and (iii) use of a gamma-labelled radioligand. The reagents are relatively ... | [
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PMID:26486 | Purification and serological studies of human alpha-L-fucosidase in the normal and fucosidosis states. | An antiserum has been raised to purified alpha-L-fucosidase. Levels of cross-reaction with serum of two unrelated fucosidosis patients and normal individuals with low activity are consistent with the presence of very low amounts of normal enzyme. Similarly no cross-reacting material could be found in cultured fibroblas... | Purification and serological studies of human alpha-L-fucosidase in the normal and fucosidosis states. An antiserum has been raised to purified alpha-L-fucosidase. Levels of cross-reaction with serum of two unrelated fucosidosis patients and normal individuals with low activity are consistent with the presence of very ... | [
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PMID:26487 | Sphingomyelinase activity levels in human peripheral blood leukocytes, using [3H]sphingomyelin as substrate: study of heterozygotes and homozygotes for Niemann-Pick disease variants. | Patients and heterozygous carriers of Niemann-Pick disease types A and B as well as the primary (genetic) sea-blue histiocyte syndrome were investigated for their leukocyte sphingomyelinase activity. In parallel, glucocerebrosidase activity was determined in all cases studied. [3H]Sphingomyelin and [14C]glucocerebrosid... | Sphingomyelinase activity levels in human peripheral blood leukocytes, using [3H]sphingomyelin as substrate: study of heterozygotes and homozygotes for Niemann-Pick disease variants. Patients and heterozygous carriers of Niemann-Pick disease types A and B as well as the primary (genetic) sea-blue histiocyte syndrome we... | [
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PMID:26488 | Serum alanine assay with an enzymic micromethod (L-alanine dehydrogenase). | L-Alanine was measured by an enzymic micromethod in serum after treatment with perchloric acid, as well as after ultrafiltration through collodium membrane filters. Serum L-alanine was also determined by an automated column chromatographic technique. Using the enzymic method, spuriously increased L-alanine levels could... | Serum alanine assay with an enzymic micromethod (L-alanine dehydrogenase). L-Alanine was measured by an enzymic micromethod in serum after treatment with perchloric acid, as well as after ultrafiltration through collodium membrane filters. Serum L-alanine was also determined by an automated column chromatographic techn... | [
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PMID:26489 | Interaction of [14C]acetylsalicylic acid with normal human peripheral blood lymphocytes. | Therapeutic concentrations of acetylsalicylic acid (ASA) have strikingly inhibited in vitro and in vivo mitogen- and antigen-induced blastogenesis by human lymphocytes. These observations may be pertinent to the anti-inflammatory actions of ASA. To investigate further the possible effects of ASA on cellular responses, ... | Interaction of [14C]acetylsalicylic acid with normal human peripheral blood lymphocytes. Therapeutic concentrations of acetylsalicylic acid (ASA) have strikingly inhibited in vitro and in vivo mitogen- and antigen-induced blastogenesis by human lymphocytes. These observations may be pertinent to the anti-inflammatory a... | [
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PMID:26493 | Clorazepate kinetics in treated epileptics. | Clorazepate is decarboxylated to form desmethyldiazepam and is a convenient way of administering it. Its kinetics were investigated in epileptic patients after single oral and multiple oral doses. Peak serum concentrations of demethyldiazepam occurred in 0.5 to 1 hr. There appeared to be a brief lag before rapid absorp... | Clorazepate kinetics in treated epileptics. Clorazepate is decarboxylated to form desmethyldiazepam and is a convenient way of administering it. Its kinetics were investigated in epileptic patients after single oral and multiple oral doses. Peak serum concentrations of demethyldiazepam occurred in 0.5 to 1 hr. There ap... | [
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PMID:26494 | Barbiturate physical dependence in mice: effects of neuroleptics and diazepam on the withdrawal syndrome. | Diazepam (8 mg/kg) quickly and effectively reduced the incidence of withdrawal symptoms in phenobarbital dependent C57BL/6J male mice. In contrast, the neuroleptic agents employed (chlorpormazine, haloperidol, or reserpine) or alpha-methyl-p-tyrosine tended to exacerbate the withdrawal syndrome. Chlorpromazine and halo... | Barbiturate physical dependence in mice: effects of neuroleptics and diazepam on the withdrawal syndrome. Diazepam (8 mg/kg) quickly and effectively reduced the incidence of withdrawal symptoms in phenobarbital dependent C57BL/6J male mice. In contrast, the neuroleptic agents employed (chlorpormazine, haloperidol, or r... | [
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PMID:26490 | The cardiovascular effects of intraventricular 5,6-dihydroxytryptamine in conscious hypertensive rats. | 1. Conscious experimental hypertensive rats injected intraventricularly with 5,6-dihydroxytryptamine (50 microgram) responded with a rapid and long-lasting (4 days) fall in blood pressure and this was accompanied by a bradycardia of similar duration. 2. The acute actions of 5,6-dihydroxytryptamine on the cardiovascular... | The cardiovascular effects of intraventricular 5,6-dihydroxytryptamine in conscious hypertensive rats. 1. Conscious experimental hypertensive rats injected intraventricularly with 5,6-dihydroxytryptamine (50 microgram) responded with a rapid and long-lasting (4 days) fall in blood pressure and this was accompanied by a... | [
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PMID:26516 | Comparative trial of two antihistamines, mequitazine and brompheniramine. | A double-blind trial was carried out in 48 patients with allergic disorders to compare the efficacy and tolerance of mequitazine and brompheniramine. Patients received either 10 mg mequitazine or 24 mg brompheniramine daily, divided into 2 doses, for 14 days. The results, analyzed from patients' answers to a questionna... | Comparative trial of two antihistamines, mequitazine and brompheniramine. A double-blind trial was carried out in 48 patients with allergic disorders to compare the efficacy and tolerance of mequitazine and brompheniramine. Patients received either 10 mg mequitazine or 24 mg brompheniramine daily, divided into 2 doses,... | [
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PMID:26517 | Comparative trial of an antihistamine, mequitazine, and placebo. | Forty patients suffering from a dermatological condition suitable for treatment with an antihistamine were studied in a double-blind randomized trial to compare the effectiveness and tolerance of mequitazine and placebo. Over a period of 2 weeks, patients received either 5 mg mequitazine twice daily or placebo. Where j... | Comparative trial of an antihistamine, mequitazine, and placebo. Forty patients suffering from a dermatological condition suitable for treatment with an antihistamine were studied in a double-blind randomized trial to compare the effectiveness and tolerance of mequitazine and placebo. Over a period of 2 weeks, patients... | [
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PMID:26518 | Double-blind clinical comparison between a gastrin-receptor antagonist, proglumide, and a histamine H2-blocker, cimetidine. | A double-blind trial was carried out in 30 patients with peptic ulcers to assess the effects of treatment with a gastrin-receptor antagonist, proglumide, compared with a histamine H2-blocker, cimetidine. Patients received either 1200 mg proglumide or 1200 mg cimetidine per day for 28 days. The results showed that both ... | Double-blind clinical comparison between a gastrin-receptor antagonist, proglumide, and a histamine H2-blocker, cimetidine. A double-blind trial was carried out in 30 patients with peptic ulcers to assess the effects of treatment with a gastrin-receptor antagonist, proglumide, compared with a histamine H2-blocker, cime... | [
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PMID:26519 | Dose-ranging study of the new beta-adrenergic antagonist nadolol in the treatment of essential hypertension. | A preliminary, single-blind, dose-ranging study was carried out in 30 patients with essential hypertension to assess the efficacy of nadolol, a new beta-adrenoceptor blocking agent without intrinsic sympathomimetic action and with an extremely long plasma half-life. After a 2-week period on placebo, patients were treat... | Dose-ranging study of the new beta-adrenergic antagonist nadolol in the treatment of essential hypertension. A preliminary, single-blind, dose-ranging study was carried out in 30 patients with essential hypertension to assess the efficacy of nadolol, a new beta-adrenoceptor blocking agent without intrinsic sympathomime... | [
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PMID:26520 | Comparison of the new beta-adrenoceptor antagonist, nadolol, and propranolol in the treatment of angina pectoris. | A randomized, double-blind study was carried out in 24 patients with stable angina pectoris to compare the efficacy of nadolol, a new beta-adrenoceptor antagonist, and propranolol. After a period on placebo, 14 patients received nadolol once daily and 10 patients propranolol 4-times daily over a 10-week dose-ranging pe... | Comparison of the new beta-adrenoceptor antagonist, nadolol, and propranolol in the treatment of angina pectoris. A randomized, double-blind study was carried out in 24 patients with stable angina pectoris to compare the efficacy of nadolol, a new beta-adrenoceptor antagonist, and propranolol. After a period on placebo... | [
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PMID:26522 | Cutaneous vasculitis. | Cutaneous vasculitis is a common but confusing clinical syndrome. We report three illustrative cases demonstrating the variable nature of the process. Renal disease is generally a poor prognostic sign; therefore, the renal status should be evaluated early. The process probably represents an immune complex disorder. Alt... | Cutaneous vasculitis. Cutaneous vasculitis is a common but confusing clinical syndrome. We report three illustrative cases demonstrating the variable nature of the process. Renal disease is generally a poor prognostic sign; therefore, the renal status should be evaluated early. The process probably represents an immune... | [
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PMID:26523 | Metabolism of 5-isopropyl-1-methyl-2-nitro-1H-imidazole. Identification of some urinary metabolites in the dog. | The metabolism of 5-isopropyl-1-methyl-2-nitro-1H-[2-14C] imidazole in dogs has been investigated after oral administration of 50 mg/kg. Three main metabolites, still containing the nitro group and accounting for about 50% of the total radiocarbon, together with a small amount of the unchanged drug, were isolated from ... | Metabolism of 5-isopropyl-1-methyl-2-nitro-1H-imidazole. Identification of some urinary metabolites in the dog. The metabolism of 5-isopropyl-1-methyl-2-nitro-1H-[2-14C] imidazole in dogs has been investigated after oral administration of 50 mg/kg. Three main metabolites, still containing the nitro group and accounting... | [
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PMID:26524 | Formation of sulfone metabolites from chlorpromazine and perazine in man. | Didesmethylchlorpromazine sulfone [gamma-(2-chlorophenothiazinyl-10)-propylamine sulfone] has been isolated from the urine of a patient under continuous chlorpromazine therapy and identified by mass spectrometry. The same compound was present in organs of rats after injection of the corresponding sulfide. The Cl-free a... | Formation of sulfone metabolites from chlorpromazine and perazine in man. Didesmethylchlorpromazine sulfone [gamma-(2-chlorophenothiazinyl-10)-propylamine sulfone] has been isolated from the urine of a patient under continuous chlorpromazine therapy and identified by mass spectrometry. The same compound was present in ... | [
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PMID:26525 | Comparison of biliary excretory function and bile composition in male, female, and lactating female rats. | The rates of excretion of phenol-3,6-dibromphthalein disulfonate, ouabain, indocyanine green, and amaranth into the bile of male and female rats were found to be similar. The rates of bile production in male and female rats were also similar whereas that of lactating rats was 50% greater. The increase in bile productio... | Comparison of biliary excretory function and bile composition in male, female, and lactating female rats. The rates of excretion of phenol-3,6-dibromphthalein disulfonate, ouabain, indocyanine green, and amaranth into the bile of male and female rats were found to be similar. The rates of bile production in male and fe... | [
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PMID:26527 | Dihydropyrimidinase. Stereochemistry of the metabolism of some 5-alkylhydantoins. | The (R)- and (S)-isomers of 5-methylhydantoin (5-MH) and of 5-isopropylhydantoin (5-IPH) were synthesized, and incubations of the individual isomers with a rat liver dihydropyrimidinase preparation (100,000g supernatant fraction) were carried out. Only the (R)-isomer of 5-MH or 5-IPH was ring-opened by the enzyme. Reve... | Dihydropyrimidinase. Stereochemistry of the metabolism of some 5-alkylhydantoins. The (R)- and (S)-isomers of 5-methylhydantoin (5-MH) and of 5-isopropylhydantoin (5-IPH) were synthesized, and incubations of the individual isomers with a rat liver dihydropyrimidinase preparation (100,000g supernatant fraction) were car... | [
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PMID:26528 | Dihydropyrimidinase. Metabolism of some cyclic imides of different ring size. | The ability of dihydropyrimidinase (EC 3.5.2.2) to hydrolyze cyclic imides of different ring size was investigated. Succinimide, glutarimide, and adipimide are five-, six-, and seven-membered cyclic imides, respectively. The ring-opened compounds that correspond to these cyclic imides are, respectively, succinamic, glu... | Dihydropyrimidinase. Metabolism of some cyclic imides of different ring size. The ability of dihydropyrimidinase (EC 3.5.2.2) to hydrolyze cyclic imides of different ring size was investigated. Succinimide, glutarimide, and adipimide are five-, six-, and seven-membered cyclic imides, respectively. The ring-opened compo... | [
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PMID:26529 | Metabolism and tissue distribution of mono-2-ethylhexyl phthalate in the rat. | The absorption, distribution and metabolic excretion of mono-2-ethylhexyl [7-14C]phthalate (MEHP) were studied in the rat. This compound was readily absorbed from the gastrointestinal tract. Radioactivity following intravenous administration of 14C-MEHP was rapidly distributed in all tissues, with the highest levels oc... | Metabolism and tissue distribution of mono-2-ethylhexyl phthalate in the rat. The absorption, distribution and metabolic excretion of mono-2-ethylhexyl [7-14C]phthalate (MEHP) were studied in the rat. This compound was readily absorbed from the gastrointestinal tract. Radioactivity following intravenous administration ... | [
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PMID:26530 | Species, sex, and developmental differences in the O- and N-dealkylation of ethylmorphine by hepatic microsomes. | 3-O-[1'-14C]Ethylmorphine and ethylmorphine, respectively, were used to measure O- and N-dealkylase activities of hepatic microsomes. The well-known sex difference in the rate of N-delakylation in mature rats was not observed with O-dealkylation, nor did O-dealkylase activity increase as male rats reached maturity, as ... | Species, sex, and developmental differences in the O- and N-dealkylation of ethylmorphine by hepatic microsomes. 3-O-[1'-14C]Ethylmorphine and ethylmorphine, respectively, were used to measure O- and N-dealkylase activities of hepatic microsomes. The well-known sex difference in the rate of N-delakylation in mature rat... | [
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PMID:26532 | Levodopa pharmacokinetics. Alterations after benserazide, a decarboxylase inhibitor. | Plasma levodopa decay curves appeared to be triexponential up to 6 hr after single intravenous injections of levodopa in rats, rabbits, and dogs. After pretreatment of each of these three species with benserazide (Ro-4-4602), a decarboxylase inhibitor, plasma levodopa concentrations declined biexponentially. Administra... | Levodopa pharmacokinetics. Alterations after benserazide, a decarboxylase inhibitor. Plasma levodopa decay curves appeared to be triexponential up to 6 hr after single intravenous injections of levodopa in rats, rabbits, and dogs. After pretreatment of each of these three species with benserazide (Ro-4-4602), a decarbo... | [
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PMID:26533 | Biotransformation products of 3,4,4'-trichlorocarbanilide in rat, monkey, and man. | 3,4,4'-Trichlorocarbanilide (TCC), uniformly labeled with 14C in the monochloro ring, was administered to rats, rhesus monkeys, and humans. Radioactive materials in the plasma and urine of all three species and in the bile of rats and monkeys were separated by high performance liquid chromatography. The chromatography ... | Biotransformation products of 3,4,4'-trichlorocarbanilide in rat, monkey, and man. 3,4,4'-Trichlorocarbanilide (TCC), uniformly labeled with 14C in the monochloro ring, was administered to rats, rhesus monkeys, and humans. Radioactive materials in the plasma and urine of all three species and in the bile of rats and mo... | [
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PMID:26534 | The absorption, excretion, and biotransformation of 3,4,4'-trichlorocarbanilide in humans. | The metabolism and disposition of 14C-TCC (3,4,4'-trichlorocarbanilide) have been evaluated in humans following oral exposure to 2.2 mumol/kg body wt. Fecal elimination (70% of dose) was complete 120 hr after dosing and the urinary excretion (27% of dose) was completed in 80 hr. The maximum plasma level occurred 2.8 hr... | The absorption, excretion, and biotransformation of 3,4,4'-trichlorocarbanilide in humans. The metabolism and disposition of 14C-TCC (3,4,4'-trichlorocarbanilide) have been evaluated in humans following oral exposure to 2.2 mumol/kg body wt. Fecal elimination (70% of dose) was complete 120 hr after dosing and the urina... | [
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PMID:26535 | Metabolism of cyclobenzaprine in the dog. | Ten metabolites of cyclobenzaprine, accounting for approximately 50% of the urinary radioactivity, were identified in the urine of dogs to which the labeled drug had been given orally. These included the 1,2-dihydrodiol, three phenolic derivatives, the N-oxide, the 10,11-epoxide, the 10,11-glycol, desmethylcyclobenzapr... | Metabolism of cyclobenzaprine in the dog. Ten metabolites of cyclobenzaprine, accounting for approximately 50% of the urinary radioactivity, were identified in the urine of dogs to which the labeled drug had been given orally. These included the 1,2-dihydrodiol, three phenolic derivatives, the N-oxide, the 10,11-epoxid... | [
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PMID:26536 | Pharmacokinetic model of presystemic metabolism. | A pharmacokinetic perfusion model is presented that describes the disposition of drugs that are subject to both first-pass hepatic and intestinal epithelial metabolism. Equations are developed to estimate hepatic and intestinal epithelial clearances by determining drug concentrations as a function of time in both porta... | Pharmacokinetic model of presystemic metabolism. A pharmacokinetic perfusion model is presented that describes the disposition of drugs that are subject to both first-pass hepatic and intestinal epithelial metabolism. Equations are developed to estimate hepatic and intestinal epithelial clearances by determining drug c... | [
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PMID:26538 | Studies on metabolism of bromazepam. VI. Reduction of 2-(2-amino-5-bromobenzoyl)pyridine, a metabolite of bromazepam, in the rabbit, rat, and guinea pig. | Three urinary metabolites that were formed by cleavage of the benzodiazepine ring of bromazepam, 2-(2-amino-5-bromobenzoyl)pyridine (ABBP), 2-(2-amino-5-bromo-3-hydroxybenzoyl)pyridine (3-OH-ABBP), and 2-amino-5-bromo-2'-azabenzhydrol (ABAB), were measured in urine of rabbits, rats, and guinea pigs. The major metabolit... | Studies on metabolism of bromazepam. VI. Reduction of 2-(2-amino-5-bromobenzoyl)pyridine, a metabolite of bromazepam, in the rabbit, rat, and guinea pig. Three urinary metabolites that were formed by cleavage of the benzodiazepine ring of bromazepam, 2-(2-amino-5-bromobenzoyl)pyridine (ABBP), 2-(2-amino-5-bromo-3-hydro... | [
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PMID:26539 | Metabolism of levorotary 4,5-dihydrodiazepam in the rat. | The metabolism of (-)-4,5-dihydrodiazepam (7-chloro-1,3,4,5-tetrahydro-1-methyl-5-phenyl-2H-1,4-benzo[2-14C]diazepin-2-one) (I) was investigated in rats. Metabolites from urine and bile extracts purified by thin-layer chromatography were identified by mass spectrometry. Diazepam and its main metabolites were found amon... | Metabolism of levorotary 4,5-dihydrodiazepam in the rat. The metabolism of (-)-4,5-dihydrodiazepam (7-chloro-1,3,4,5-tetrahydro-1-methyl-5-phenyl-2H-1,4-benzo[2-14C]diazepin-2-one) (I) was investigated in rats. Metabolites from urine and bile extracts purified by thin-layer chromatography were identified by mass spectr... | [
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PMID:26541 | Microsomal N-hydroxylation of trans-4'-alkoxy-4-acetamidostilbenes. | Hamster liver microsomes catalyze the N-hydroxylation of the 4'-OCH3, 4'-OCH2CH3, 4'-O(CH2)2CH3, and 4'-O(CH2)3CH3 analogs of trans-4-acetamidostilbene. Other metabolites which were identified were the O-deethylation product of the 4'-OCH2CH3 analog as well as the alpha,beta-epoxides of the 4'-OCH2CH3 and 4'-O(CH2)2CH3... | Microsomal N-hydroxylation of trans-4'-alkoxy-4-acetamidostilbenes. Hamster liver microsomes catalyze the N-hydroxylation of the 4'-OCH3, 4'-OCH2CH3, 4'-O(CH2)2CH3, and 4'-O(CH2)3CH3 analogs of trans-4-acetamidostilbene. Other metabolites which were identified were the O-deethylation product of the 4'-OCH2CH3 analog as... | [
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PMID:26542 | Microsomal mixed-function amine oxidase. Oxidation products of piperazine-substituted phenothiazine drugs. | Oxidation products of fluphenazide, thioproperazine, and trifluoperazine obtained in reactions catalyzed by homogeneous preparations of the microsomal mixed-function amine oxidase have been isolated and identified. Approximately 0.5 g of metabolite of each piperazine-substituted phenothiazine drug was prepared in react... | Microsomal mixed-function amine oxidase. Oxidation products of piperazine-substituted phenothiazine drugs. Oxidation products of fluphenazide, thioproperazine, and trifluoperazine obtained in reactions catalyzed by homogeneous preparations of the microsomal mixed-function amine oxidase have been isolated and identified... | [
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PMID:26544 | Influence of pregnancy and folic acid on phenytoin metabolism by rat liver microsomes. | Liver microsomal suspensions from pregnant and nonpregnant Sprague-Dawley rats were assayed for NADPH-dependent metabolism of phenytoin to the hydroxylated products, 5-(rho-hydroxyphenyl)-5-phenylhydantoin (rhoHPPH) and 5-(3,4-dihydroxy-1,5-cyclohexadien-1-yl)5-phenylhydantoin (H2DIOL). UDP-glucuronic acid-dependent gl... | Influence of pregnancy and folic acid on phenytoin metabolism by rat liver microsomes. Liver microsomal suspensions from pregnant and nonpregnant Sprague-Dawley rats were assayed for NADPH-dependent metabolism of phenytoin to the hydroxylated products, 5-(rho-hydroxyphenyl)-5-phenylhydantoin (rhoHPPH) and 5-(3,4-dihydr... | [
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PMID:26550 | Quantitation of N-demethylantipyrine in biological samples and isolation and characterization of its glucuronic acid conjugate. | An improved method for quantitating N-demethylantipyrine (N-DEM-AP) in urine by gas chromatography or gas chromatography-mass spectrometry has been developed. Recovery of greater than 90% of N-DEM-AP was achieved by extraction of the sample at pH 1 after addition of 3-amino-1-phenyl-2-pyrazolin-5-one. The coefficient o... | Quantitation of N-demethylantipyrine in biological samples and isolation and characterization of its glucuronic acid conjugate. An improved method for quantitating N-demethylantipyrine (N-DEM-AP) in urine by gas chromatography or gas chromatography-mass spectrometry has been developed. Recovery of greater than 90% of N... | [
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PMID:26549 | Alterations in the pharmacokinetics of 3H-delta9-tetrahydrocannabinol in mice by bacterial endotoxin. | Mice were pretreated with either bacterial endotoxin (3 mg/kg, ip) or saline 3 hr prior to an ip injection of 100 mg of 3H-delta9-tetrahydrocannabinol (3H-delta9-THC) per kg, a combination that results in synergistic lethality. Five hours after the injection of 3H-delta9-THC, the endotoxin-pretreated mice contained a s... | Alterations in the pharmacokinetics of 3H-delta9-tetrahydrocannabinol in mice by bacterial endotoxin. Mice were pretreated with either bacterial endotoxin (3 mg/kg, ip) or saline 3 hr prior to an ip injection of 100 mg of 3H-delta9-tetrahydrocannabinol (3H-delta9-THC) per kg, a combination that results in synergistic l... | [
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PMID:26552 | The metabolism of (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid in chimpanzee and man. | The metabolism of the polyvalent saluretic agent (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid was studied in chimpanzee and man. The drug was well absorbed and extensively metabolized by man. Peak levels of drug (5--8 microgram/ml) occurred within 1.5--4.5 hr of drug administration. The plasma ha... | The metabolism of (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid in chimpanzee and man. The metabolism of the polyvalent saluretic agent (2-cyclopentyl-6,7-dichloro-2-methyl-1-oxo-5-indanyloxy)acetic acid was studied in chimpanzee and man. The drug was well absorbed and extensively metabolized by m... | [
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PMID:26551 | Urinary metabolites of 3,5-di-(1-[13C]methyl-1-methylethyl)4-hydroxytoluene (BHT-13C) in man. | Butylated hydroxytoluene (BHT) containing the stable isotope 13C was synthesized from 2-[13C]methylpropan-2-ol. A minor constituent of urine following ingestion of BHT-13C by a human volunteer was identified as 3,5-di-(1-[13C]methyl-1-methylethyl)-4-hydroxybenzoic acid, The major metabolite detected was 13C-labeled 5-c... | Urinary metabolites of 3,5-di-(1-[13C]methyl-1-methylethyl)4-hydroxytoluene (BHT-13C) in man. Butylated hydroxytoluene (BHT) containing the stable isotope 13C was synthesized from 2-[13C]methylpropan-2-ol. A minor constituent of urine following ingestion of BHT-13C by a human volunteer was identified as 3,5-di-(1-[13C]... | [
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PMID:26554 | Elimination of radioactivity following administration of [15,16-3H]naltrexone to rats and guinea pigs. | The elimination of radioactivity after [15,16-3H]naltrexone administration was studied in rats and guinea pigs. An average of 42% of the dose was eliminated in urine and 55% in feces following administration of 1 mg/kg iv to each of three rats. Analysis of radioactivity in the excreta of one rat that received the same ... | Elimination of radioactivity following administration of [15,16-3H]naltrexone to rats and guinea pigs. The elimination of radioactivity after [15,16-3H]naltrexone administration was studied in rats and guinea pigs. An average of 42% of the dose was eliminated in urine and 55% in feces following administration of 1 mg/k... | [
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PMID:26555 | Lipid-soluble inhibitors of dihydrofolate reductase. I. Kinetics, tissue distribution, and extent of metabolism of pyrimethamine, metoprine, and etoprine in the rat, dog, and man. | With the aim of developing anticancer compounds which overcome some of the clinical limitations of the polar dihydrofolate reductase inhibitor, methotrexate, the physicochemical properties, kinetics, and metabolism of a series of lipid-soluble 2,4-diamino-5-phenylpyrimidine folate antagonists have been studied. Metopri... | Lipid-soluble inhibitors of dihydrofolate reductase. I. Kinetics, tissue distribution, and extent of metabolism of pyrimethamine, metoprine, and etoprine in the rat, dog, and man. With the aim of developing anticancer compounds which overcome some of the clinical limitations of the polar dihydrofolate reductase inhibit... | [
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PMID:26559 | [Assessment of vigilance]. | Two aspects of vigilance are to be distinguished: the quantitative one refers to sleep-wakefulness dimension and the qualitative one refers to focusing of attention. Their combination leads to a curvilinear relationship between activation and performances. After describing the psychometric characteristics of vigilance ... | [Assessment of vigilance]. Two aspects of vigilance are to be distinguished: the quantitative one refers to sleep-wakefulness dimension and the qualitative one refers to focusing of attention. Their combination leads to a curvilinear relationship between activation and performances. After describing the psychometric ch... | [
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PMID:26556 | Pharmacokinetics and steady-state myocardial uptake of disopyramide in the dog. | The pharmacokinetics and steady-state myocardial uptake of the antiarrhythmic drug disopyramide (DP) were determined in dogs after oral or intravenous administration of [14C]disopyramide phosphate. DP was absorbed rapidly and its absolute oral bioavailability was about 70%. Significant dose-dependent kinetics were not ... | Pharmacokinetics and steady-state myocardial uptake of disopyramide in the dog. The pharmacokinetics and steady-state myocardial uptake of the antiarrhythmic drug disopyramide (DP) were determined in dogs after oral or intravenous administration of [14C]disopyramide phosphate. DP was absorbed rapidly and its absolute o... | [
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PMID:26560 | [Influence of pipotiazine on schizophrenia]. | This study is an account of thirty cases of schizophrenia treated experimentally in open with Pipotiazine (19366 R.P.), these cases, of the Kraepelin's Dementia Praecox type, in serious or complicated forms necessitating important measures of hospital care. The quantitative and qualitative therapeutic results, very fav... | [Influence of pipotiazine on schizophrenia]. This study is an account of thirty cases of schizophrenia treated experimentally in open with Pipotiazine (19366 R.P.), these cases, of the Kraepelin's Dementia Praecox type, in serious or complicated forms necessitating important measures of hospital care. The quantitative ... | [
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PMID:26561 | Chorismate mutase/prephenate dehydratase from Escherichia coli K12. Effect of phenylalanine, NaCl and pH on the protein conformation. | The effects of phenylalanine, NaCl and pH on the conformation of chorismate mutase/prephenate dehydratase have been investigated, using measurements of far and near-ultraviolet circular dichroic spectra and ultraviolet difference spectra. At pH 8.2 in 20 mM Tris-Cl buffer the enzyme was found to contain 10-20% helix an... | Chorismate mutase/prephenate dehydratase from Escherichia coli K12. Effect of phenylalanine, NaCl and pH on the protein conformation. The effects of phenylalanine, NaCl and pH on the conformation of chorismate mutase/prephenate dehydratase have been investigated, using measurements of far and near-ultraviolet circular ... | [
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PMID:26562 | Chorismate mutase/prephenate dehydratase from Escherichia coli K12. Binding studies with the allosteric effector phenylalanine. | The binding of phenylalanine to the allosteric site of chorismate mutase/prephenate dehydratase has been studied by steady-state dialysis. Under most of the experimental conditions examined positive co-operativity was observed for the binding of ligand up to 50% saturation and negative co-operativity above 50% saturati... | Chorismate mutase/prephenate dehydratase from Escherichia coli K12. Binding studies with the allosteric effector phenylalanine. The binding of phenylalanine to the allosteric site of chorismate mutase/prephenate dehydratase has been studied by steady-state dialysis. Under most of the experimental conditions examined po... | [
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PMID:26564 | Kinetics of the interaction of alpha-chymotrypsin with trypsin kallikrein inhibitor (Kunitz) in which the reactive-site peptide bond Lys-15--Ala-16 is split. | Modified trypsin kallikrein inhibitor (I*), with the reactive-site peptide bond Lys-15--Ala-16 split, reacts with alpha-chymotrypsin (E) via an intermediate X to the stable tetrahedral complex C:E + I in equilibrium X leads to C. Formation X constitutes a fast pre-equilibrium (equilibrium constant Kx = 7 X 10(-5) M, a... | Kinetics of the interaction of alpha-chymotrypsin with trypsin kallikrein inhibitor (Kunitz) in which the reactive-site peptide bond Lys-15--Ala-16 is split. Modified trypsin kallikrein inhibitor (I*), with the reactive-site peptide bond Lys-15--Ala-16 split, reacts with alpha-chymotrypsin (E) via an intermediate X to ... | [
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PMID:26567 | Cycloheximide causes increased accumulation of translatable mRNA for tyrosine aminotransferase and tryptophan oxygenase in livers of cortisol-treated rats. | Messenger RNA activities for two cortisol-inducible enzymes, tyrosine aminotransferase and tryptophan oxygenase, have been determined by translation in a wheat germ system. The effects of cycloheximide on the two mRNA activities have been evaluated. Cortisol leads to an increase of the translatable mRNAs for tyrosine a... | Cycloheximide causes increased accumulation of translatable mRNA for tyrosine aminotransferase and tryptophan oxygenase in livers of cortisol-treated rats. Messenger RNA activities for two cortisol-inducible enzymes, tyrosine aminotransferase and tryptophan oxygenase, have been determined by translation in a wheat germ... | [
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PMID:26570 | Formation of complexes between microsomal cytochrome P-450-Fe(II) and nitrosoarenes obtained by oxidation of arylhydroxylamines or reduction of nitroarenes in situ. | A cytochrome P-450 complex exhibiting a Soret peak at 454 nm is formed by direct interaction of nitrosobenzene with NADPH-reduced rat liver microsomes in anaerobic conditions, by reaction of phenylhydroxylamine with aerobic microsomes or during nitrobenzene reduction by NADPH-reduced or dithionite-reduced microsomes. I... | Formation of complexes between microsomal cytochrome P-450-Fe(II) and nitrosoarenes obtained by oxidation of arylhydroxylamines or reduction of nitroarenes in situ. A cytochrome P-450 complex exhibiting a Soret peak at 454 nm is formed by direct interaction of nitrosobenzene with NADPH-reduced rat liver microsomes in a... | [
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PMID:26572 | Neurotransmittor changes in the rat brain after portacaval anastomosis. | Portacaval anastomosis in rats elevated the brain serotonin content by about 30%, the greatest increase being noted in the brain stem. A minor increase in norepinephrine content but no change in dopamine concentration was also noted. Low dose L-dopa treatment reversed the serotonin changes but did not affect catecholam... | Neurotransmittor changes in the rat brain after portacaval anastomosis. Portacaval anastomosis in rats elevated the brain serotonin content by about 30%, the greatest increase being noted in the brain stem. A minor increase in norepinephrine content but no change in dopamine concentration was also noted. Low dose L-dop... | [
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PMID:26573 | Effect of capsule colour and order of administration of hypnotic treatments. | Ninety-six hospitalized insomniac patients were asked to compare by a daily questionnaire the effect on sleep of the colour of the capsules and the order of administration of two treatments--heptabarbital and placebo. A balanced incomplete-block design was used; sleep onset time and sleep duration time were the main cr... | Effect of capsule colour and order of administration of hypnotic treatments. Ninety-six hospitalized insomniac patients were asked to compare by a daily questionnaire the effect on sleep of the colour of the capsules and the order of administration of two treatments--heptabarbital and placebo. A balanced incomplete-blo... | [
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PMID:26575 | Subpopulations of mouse T lymphocytes. II. Suppression of graft-vs.-host reactions by naturally proliferating splenic T cells. | The immunological role of a naturally proliferating subpopulation of splenic T cells was investigated using the graft-vs.-host (GvH) reaction on the mouse. Normal parental spleen cells, purified splenic T cells or lymph node cells were pulse-treated for one hour in vitro with tritiated thymidine of high specific activi... | Subpopulations of mouse T lymphocytes. II. Suppression of graft-vs.-host reactions by naturally proliferating splenic T cells. The immunological role of a naturally proliferating subpopulation of splenic T cells was investigated using the graft-vs.-host (GvH) reaction on the mouse. Normal parental spleen cells, purifie... | [
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PMID:26576 | Investigation of cardiac beta-adrenoceptors using 125I-labelled 1-(4-iodophenoxy)-3-isopropylaminopropan-2-ol. | 1-(4-iodophenoxy)-3-isopropylaminopropan-2-ol (IIP) is a potent beta-adrenergic antagonist which has been labelled to high specific activity with 125I and used to bind to rat myocardial membranes. The characteristics of binding were consistent with the known properties of beta-receptors. Thus, binding was highly stereo... | Investigation of cardiac beta-adrenoceptors using 125I-labelled 1-(4-iodophenoxy)-3-isopropylaminopropan-2-ol. 1-(4-iodophenoxy)-3-isopropylaminopropan-2-ol (IIP) is a potent beta-adrenergic antagonist which has been labelled to high specific activity with 125I and used to bind to rat myocardial membranes. The characte... | [
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PMID:26577 | Benzodiazepines: potentiation of a GABA inhibitory response in the dorsal raphe nucleus. | Based on evidence that the dorsal raphe nucleus (DR) has specific and independent receptors for 5HT, GABA and glycine (Gallager and Aghajanian, 1976; Wang and Aghajanian, 1977), alterations in the firing rate of DR neurons following the administration of benzodiazepines (BZ) were evaluated to determine whether they wer... | Benzodiazepines: potentiation of a GABA inhibitory response in the dorsal raphe nucleus. Based on evidence that the dorsal raphe nucleus (DR) has specific and independent receptors for 5HT, GABA and glycine (Gallager and Aghajanian, 1976; Wang and Aghajanian, 1977), alterations in the firing rate of DR neurons followin... | [
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PMID:26578 | 2,5-Dimethoxy-4-methylamphetamine (DOM)- a central component of its cardiovascular effects in rats; involvement of serotonin. | The hallucinogen DOM produces a rise in blood pressure and heart rate when injected into the cerebral ventricles of anesthetized rats. These effects are abolished in rats with transected spinal cords but are unaffected by prior treatment with hexamethonium. Central but not peripheral administration of the serotonin ant... | 2,5-Dimethoxy-4-methylamphetamine (DOM)- a central component of its cardiovascular effects in rats; involvement of serotonin. The hallucinogen DOM produces a rise in blood pressure and heart rate when injected into the cerebral ventricles of anesthetized rats. These effects are abolished in rats with transected spinal ... | [
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PMID:26579 | Biphasic effect of chlorpromazine on rat paradoxical sleep: a study of dose-related mechanisms. | The experiments reported here investigated the effect of chlorpromazine (CPZ) alone or after inhibition of catecholamine (CA) synthesis on paradoxical sleep (PS) in the rat. The dose--response curve for CPZ was biphasic with enhancement of PS after low doses, and depression of PS after higher doses. In contrast, low do... | Biphasic effect of chlorpromazine on rat paradoxical sleep: a study of dose-related mechanisms. The experiments reported here investigated the effect of chlorpromazine (CPZ) alone or after inhibition of catecholamine (CA) synthesis on paradoxical sleep (PS) in the rat. The dose--response curve for CPZ was biphasic with... | [
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PMID:26580 | Studies on the mechanism of the vasodilator effects of prazosin in dogs and rabbits. | In pentobarbital (35.0 mg/kg) anaesthetised dogs, bolus injections of prazosin into the femoral artery (3.0--300.0 microgram) provoked a dose-related fall in the vascular resistance of the innervated hind limb. In contrast to papaverine, prazosin failed to produce the same effect in dogs under spinal anaesthesia even w... | Studies on the mechanism of the vasodilator effects of prazosin in dogs and rabbits. In pentobarbital (35.0 mg/kg) anaesthetised dogs, bolus injections of prazosin into the femoral artery (3.0--300.0 microgram) provoked a dose-related fall in the vascular resistance of the innervated hind limb. In contrast to papaverin... | [
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PMID:26581 | Positive chronotropic and inotropic responses to guanosine in the isolated dog atrium. | The effects of guanosine on chronotropism and inotropism in isolated dog atria were studied in spontaneously beating preparations which were suspended in a bath perfused with arterial blood from a carotid artery of a heparinized support dog. Guanosine administered into the cannulated sinus node artery in a dose range o... | Positive chronotropic and inotropic responses to guanosine in the isolated dog atrium. The effects of guanosine on chronotropism and inotropism in isolated dog atria were studied in spontaneously beating preparations which were suspended in a bath perfused with arterial blood from a carotid artery of a heparinized supp... | [
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PMID:26584 | Graft versus leukemia. VIII. Selective reduction in antihost reactivity without loss of antileukemic reactivity by treatment of donor mice with lipopolysaccharide. | Spleen and lymph node cells from DBA/2 (H-2d) donor mice treated with multiple injections of bacterial lipopolysaccharide (LPS) were tested in vivo for reactivity against normal tissues of host AKR (H-2k) mice against an AKR long-passage, acute lymphoblastic leukemia (BW5147). LPS treatment of donor mice resulted in a ... | Graft versus leukemia. VIII. Selective reduction in antihost reactivity without loss of antileukemic reactivity by treatment of donor mice with lipopolysaccharide. Spleen and lymph node cells from DBA/2 (H-2d) donor mice treated with multiple injections of bacterial lipopolysaccharide (LPS) were tested in vivo for reac... | [
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PMID:26587 | Acid release at meiotic maturation of oocytes in the polychaete annelid Sabellaria alveolata. | ABout 1 pmole of acid per egg is released when prophasic oocytes undergo maturation under the action of sperm, proteases or ionophore A 23187. No similar acid release occurs at fertilization of matured oocytes. These findings are compared with data on Urechis and sea urchin. | Acid release at meiotic maturation of oocytes in the polychaete annelid Sabellaria alveolata. ABout 1 pmole of acid per egg is released when prophasic oocytes undergo maturation under the action of sperm, proteases or ionophore A 23187. No similar acid release occurs at fertilization of matured oocytes. These findings ... | [
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PMID:26588 | [Effect of tropaphene and fentolamin on the spasmogenic effects of adrenaline, noradrenaline, serotonin and other biologically active substances]. | Tests conducted in vitro and in vivo demonstrated that tropaphen, tropine ether of alpha-phenyl-beta-(p-acetoxyphenyl)-propionic acid, an original alpha-adrenoblocking agent, display a marked antiserotonin activity exceeding that of phentolamine. Moreover, tropaphen is more active that phenolamine by its inhibiting inf... | [Effect of tropaphene and fentolamin on the spasmogenic effects of adrenaline, noradrenaline, serotonin and other biologically active substances]. Tests conducted in vitro and in vivo demonstrated that tropaphen, tropine ether of alpha-phenyl-beta-(p-acetoxyphenyl)-propionic acid, an original alpha-adrenoblocking agent... | [
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PMID:26589 | [Comparative assessment of the effect of sympatholytics and beta-adrenoblockaders on carbohydrate-phosphorus metabolic indices in the myocardium of growing rats]. | The sympatholyitic ornide and beta-adrenoblocking agent alpheprol were introduced intraperitoneally in single doses of 5 and 1 mg/kg, respectively to 7--30 day and 3--5-month old adult rats. The content of ATP, ADP, AMP, inorganic phosphorus glycogen and also active P32 incorporation were determined. The 7-day old ratt... | [Comparative assessment of the effect of sympatholytics and beta-adrenoblockaders on carbohydrate-phosphorus metabolic indices in the myocardium of growing rats]. The sympatholyitic ornide and beta-adrenoblocking agent alpheprol were introduced intraperitoneally in single doses of 5 and 1 mg/kg, respectively to 7--30 d... | [
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PMID:26591 | [Metabolic effects of ethyl alcohol the ways to correct them]. | Tests conducted on albino male-rats demonstrated that with its intragastric administration in a dose of 3 g/kg ethanol produces a hypoxy-like situation in the organism, i.e. the oxygen tension in the liver and skeletal muscles decreases and the redox potential is activation during the 1st hour with succinate-cytochrome... | [Metabolic effects of ethyl alcohol the ways to correct them]. Tests conducted on albino male-rats demonstrated that with its intragastric administration in a dose of 3 g/kg ethanol produces a hypoxy-like situation in the organism, i.e. the oxygen tension in the liver and skeletal muscles decreases and the redox potent... | [
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PMID:26594 | [Ethological analysis of the action of medazepam and diazepam on the zoosocial behavior of isolated mice]. | Tests set up with isolated mice of two groups (aggressive and "fearful") evidenced that diazepam and medazepam weaken the behavioral manifestations of the partner's avoidance, increase sociability in "fearful" mice and help to regain the ability for elementary intraspecies contacts. These drugs have a biphasic action o... | [Ethological analysis of the action of medazepam and diazepam on the zoosocial behavior of isolated mice]. Tests set up with isolated mice of two groups (aggressive and "fearful") evidenced that diazepam and medazepam weaken the behavioral manifestations of the partner's avoidance, increase sociability in "fearful" mic... | [
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PMID:26590 | [Effect of a new central adrenolytic on cardiac metabolic indices in neurogenic damage]. | It is shown that in rabbits subjected to an electric stimulation of the aortic arch there developed concurrently with depletion of tissular norepinephrine reserves in the myocardium also gross metabolic disorders. A preliminary introduction of the drug izm-611 by blocking central alpha-adrenoreseptors at the same time ... | [Effect of a new central adrenolytic on cardiac metabolic indices in neurogenic damage]. It is shown that in rabbits subjected to an electric stimulation of the aortic arch there developed concurrently with depletion of tissular norepinephrine reserves in the myocardium also gross metabolic disorders. A preliminary int... | [
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PMID:26595 | [Action of analeptics in acute alcoholic intoxication]. | Tests conducted on rabbits in a state of acute ethanol poisoning (2.5 g/kg per os) of a medium degree demonstrated that caffein (10 mg/kg) and bemegride (5 mg/kg) introduced one time intravenously at the height of alcoholic intoxication raise the activity of aerobic oxidative processes, but fail to eliminate metabolic ... | [Action of analeptics in acute alcoholic intoxication]. Tests conducted on rabbits in a state of acute ethanol poisoning (2.5 g/kg per os) of a medium degree demonstrated that caffein (10 mg/kg) and bemegride (5 mg/kg) introduced one time intravenously at the height of alcoholic intoxication raise the activity of aerob... | [
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PMID:26596 | [Pharmacokinetics of the new Soviet, tritium-labelled, antihistamine preparation, phencarol]. | As evidenced no less than 45 per cent of tritium-labelled antihistaminic drug phencarol (quinuclidine-3-diphenylcarbinol hydrochloride) introduced intragastrically to rats is absorbed. The maximal radioactivity in various organs is reached in 1--3 hours, with high specific radioactivity being recorded in the lungs and ... | [Pharmacokinetics of the new Soviet, tritium-labelled, antihistamine preparation, phencarol]. As evidenced no less than 45 per cent of tritium-labelled antihistaminic drug phencarol (quinuclidine-3-diphenylcarbinol hydrochloride) introduced intragastrically to rats is absorbed. The maximal radioactivity in various orga... | [
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PMID:26597 | [Effect of amisyl and spasmolytin on the blood supply and oxygen metabolism of the brain]. | The effect of benactyzine and spasmolytin adiphenine on the blood circulation in the oxygen consumption by the brain were investigated in experiments on dogs. The resulting data point to a biphasic action of benacyzine and spasmolytin on the blood supply of the brain (after a short-lived increase of the blood flow a cl... | [Effect of amisyl and spasmolytin on the blood supply and oxygen metabolism of the brain]. The effect of benactyzine and spasmolytin adiphenine on the blood circulation in the oxygen consumption by the brain were investigated in experiments on dogs. The resulting data point to a biphasic action of benacyzine and spasmo... | [
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PMID:26598 | [Possible neuropharmacological regulation of chemical carcinogenesis caused by diethylnitrosamine]. | The effect of a number of neurotropic drugs on diethylnitrosoamine (DENA)-induced chemical carcinogenesis was studied by applying pharmacological, morphological and biochemical techniques. Atropine stimulated significantly the rat liver and esophagus carcinogenesis, whereas the alpha-adrenoblocking agent, a pyrrhoxane ... | [Possible neuropharmacological regulation of chemical carcinogenesis caused by diethylnitrosamine]. The effect of a number of neurotropic drugs on diethylnitrosoamine (DENA)-induced chemical carcinogenesis was studied by applying pharmacological, morphological and biochemical techniques. Atropine stimulated significant... | [
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PMID:26606 | The pathophysiology of hyperprolactinemic states and the role of newer ergot compounds in their treatment. | Studies of prolactin secretion in humans have confirmed the concept, derived originally from animal investigations, that prolactin is predominantly controlled by tonic inhibition from the hypothalamus. The locus of action of dopamine and dopaminergic agents such as the ergot alkaloids inhibiting prolactin secretion app... | The pathophysiology of hyperprolactinemic states and the role of newer ergot compounds in their treatment. Studies of prolactin secretion in humans have confirmed the concept, derived originally from animal investigations, that prolactin is predominantly controlled by tonic inhibition from the hypothalamus. The locus o... | [
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PMID:26609 | Evaluation of testicular function in prepubertal boys by means of the luteinizing hormone-releasing hormone test. | Luteinizing hormone (LH)-releasing hormone (LH-RH) tests (50 microgram/sq m intravenously) were performed in 112 prepubertal boys ages 13/12 to 11 years (mean +/- standard deviation, 75/12 +/- 16/12 years) suspected of having a testicular disorder because of improperly located testes (77 boys) or hypogonadism (35 boys)... | Evaluation of testicular function in prepubertal boys by means of the luteinizing hormone-releasing hormone test. Luteinizing hormone (LH)-releasing hormone (LH-RH) tests (50 microgram/sq m intravenously) were performed in 112 prepubertal boys ages 13/12 to 11 years (mean +/- standard deviation, 75/12 +/- 16/12 years) ... | [
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PMID:26611 | [Modulation of autonomic correlates of emotional stress and adaptive responses]. | The character and dynamics of the cardio-vascular response to psychogenic stress (confrontation of cat and dog) depends on active or passive type of behavioral response. Tranquilizers inhibit long-lasting hypertension otherwise occurring after the stress stimulus. Adaptive cardio-vascular responses and baroreceptor ref... | [Modulation of autonomic correlates of emotional stress and adaptive responses]. The character and dynamics of the cardio-vascular response to psychogenic stress (confrontation of cat and dog) depends on active or passive type of behavioral response. Tranquilizers inhibit long-lasting hypertension otherwise occurring a... | [
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PMID:26612 | Local graft-versus-host reaction in mice evoked by Peyer's patch and other lymphoid tissue cells tested in a lymphocyte-induced angiogenesis assay. | The competence of murine Peyer's patch cells to evoke a local GVH reaction was compared with that displayed by lymphoid cells of spleen, lymph nodes, thymus, bone marrow, peritoneal cavity and peripheral blood. The local GVH reaction was assessed in a lymphocyte-induced angiogenesis assay in which an intradermal inject... | Local graft-versus-host reaction in mice evoked by Peyer's patch and other lymphoid tissue cells tested in a lymphocyte-induced angiogenesis assay. The competence of murine Peyer's patch cells to evoke a local GVH reaction was compared with that displayed by lymphoid cells of spleen, lymph nodes, thymus, bone marrow, p... | [
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PMID:26613 | Serum polyphenol oxidase activity (ceruloplasmin) in conventional laboratory animals and man. | The optimum pH for ceruloplasmin as polyphenol oxidase (EC 1.10.3.2) activity was determined in human serum (pH 5.4) and the serum of conventional laboratory animals--the rat (pH 5.2), mouse (pH 5.2), hamster (pH 5.3), guinea pig (pH 5.4), multimammate mouse (pH 5.2) and rabbit (pH 5.4). Determined at the optimum pH in... | Serum polyphenol oxidase activity (ceruloplasmin) in conventional laboratory animals and man. The optimum pH for ceruloplasmin as polyphenol oxidase (EC 1.10.3.2) activity was determined in human serum (pH 5.4) and the serum of conventional laboratory animals--the rat (pH 5.2), mouse (pH 5.2), hamster (pH 5.3), guinea ... | [
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PMID:26614 | Evaluation of in vitro and in vivo activities of isoantibodies directed against idiotypes and recognition structures for transplantation antigens. | Anti-idiotype sera were prepared by injection of CBA anti-A/JAX serum with or without adjuvant into CBA mice. These sera were tested in allocluster inhibition and passive enhancement-facilitation. While the anti-idiotype sera inhibited allocluster formation, particularly when prepared with complete Freund's adjuvant, t... | Evaluation of in vitro and in vivo activities of isoantibodies directed against idiotypes and recognition structures for transplantation antigens. Anti-idiotype sera were prepared by injection of CBA anti-A/JAX serum with or without adjuvant into CBA mice. These sera were tested in allocluster inhibition and passive en... | [
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PMID:26620 | Interaction of glucocorticoid receptors from lymphoid cell lines with their nuclear acceptor sites. | Procedures have been developed which provide simple means of determining binding constants of steroid receptors for glucocorticoids in mouse lymphoid cell lines and of characterizing the interaction of the steroid--receptor complex with the nucleus. An average of 70% of the steroid--receptor complexes is found associat... | Interaction of glucocorticoid receptors from lymphoid cell lines with their nuclear acceptor sites. Procedures have been developed which provide simple means of determining binding constants of steroid receptors for glucocorticoids in mouse lymphoid cell lines and of characterizing the interaction of the steroid--recep... | [
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... |
PMID:26626 | Effect of cimetidine on ion fluxes and potential difference across the human stomach. | The H(2)-receptor antagonist, cimetidine, reduces acid output regardless of the means of stimulation. It is not known in man whether this is due entirely to a reduction in acid secretion or whether increased back diffusion of hydrogen ions is also occurring. We studied fluxes of H(+), Na(+), K(+), and Cl(-) ions after ... | Effect of cimetidine on ion fluxes and potential difference across the human stomach. The H(2)-receptor antagonist, cimetidine, reduces acid output regardless of the means of stimulation. It is not known in man whether this is due entirely to a reduction in acid secretion or whether increased back diffusion of hydrogen... | [
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PMID:26627 | p-Nitrobenzyl p-toluenesulfonyl-L-arginine: a chromogenic substrate for thrombin, plasmin and trypsin. | p-Nitrobenzyl p-toluenesulfonyl-L-arginine is hydrolyzed by thrombin, plasmin, and trypsin to p-nitrobenzyl alcohol and tosyl-L-arginine. The absorption of p-nitrobenzyl alcohol formed is measured at 271 nm (AmM 8.89). With 0.10 mM of the ester in 0.1 M Tris-HCl at pH 8.4 and 30 degrees C, the hydrolysis catalyzed by t... | p-Nitrobenzyl p-toluenesulfonyl-L-arginine: a chromogenic substrate for thrombin, plasmin and trypsin. p-Nitrobenzyl p-toluenesulfonyl-L-arginine is hydrolyzed by thrombin, plasmin, and trypsin to p-nitrobenzyl alcohol and tosyl-L-arginine. The absorption of p-nitrobenzyl alcohol formed is measured at 271 nm (AmM 8.89)... | [
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PMID:26628 | Chromogenic substrate assay of plasma prekallikrein. With a note on its site of biosynthesis. | A method for assaying plasma prekallikrein has been developed applying the chromogenic substrate Chromozym PK. Different variables have been investigated, and the final assay system was found to give a reproducible and reliable assay procedure. A normal value of 99.0 +/- 18% was found, the coefficient of variation bein... | Chromogenic substrate assay of plasma prekallikrein. With a note on its site of biosynthesis. A method for assaying plasma prekallikrein has been developed applying the chromogenic substrate Chromozym PK. Different variables have been investigated, and the final assay system was found to give a reproducible and reliabl... | [
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PMID:26629 | Methods for determination of prekallikrein in plasma, glandular kallikrein and urokinase. | New chromogenic tripeptide substrates have been used for the determination of kallikreins and urokinase. The conditions have been optimized. It is possible to determine prekallikrein in plasma after activation with Cephotest. No significant loss in activity caused by plasma kallikrein inhibitors is observed at the dilu... | Methods for determination of prekallikrein in plasma, glandular kallikrein and urokinase. New chromogenic tripeptide substrates have been used for the determination of kallikreins and urokinase. The conditions have been optimized. It is possible to determine prekallikrein in plasma after activation with Cephotest. No s... | [
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PMID:26631 | [Regional myocardial blood supply in coronary disease]. | 1. Value and limitations of the precordial Xenon-clearance technique are analyzed. The results of this technique are compared to the scintigraphic display of the initial Xenon distribution and to microsphere scintigraphy (Engel et al. 1976a). 2. The effects of coronary obstructions and of segmental LV dysfunction on re... | [Regional myocardial blood supply in coronary disease]. 1. Value and limitations of the precordial Xenon-clearance technique are analyzed. The results of this technique are compared to the scintigraphic display of the initial Xenon distribution and to microsphere scintigraphy (Engel et al. 1976a). 2. The effects of cor... | [
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PMID:26632 | [On the acute toxicity of labetalol (AH-5158), a combined alpha-and-beta-adrenoceptor-blocking agent (author's transl)]. | Acute toxicity studies in labetalol were performed using mice, rats and rabbits, An oral administration of labetalol produced an increase in salivary secretion due to local irritation. Death followed convulsions by large doses of labetalol. Pathological examinations suggested that the cause of death by labetalol was ci... | [On the acute toxicity of labetalol (AH-5158), a combined alpha-and-beta-adrenoceptor-blocking agent (author's transl)]. Acute toxicity studies in labetalol were performed using mice, rats and rabbits, An oral administration of labetalol produced an increase in salivary secretion due to local irritation. Death followed... | [
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PMID:26633 | Gastric lesions in familial adenomatosis coli: their incidence and histologic analysis. | In order to detect accompanying gastric lesions, we examined 22 patients with familial adenomatosis of the colon belonging to 14 families. Various gastric lesions were confirmed in 15 patients (68.2 per cent) belonging to 13 families. The lesions were found histologically to be adenoma in nine cases, fundic gland polyp... | Gastric lesions in familial adenomatosis coli: their incidence and histologic analysis. In order to detect accompanying gastric lesions, we examined 22 patients with familial adenomatosis of the colon belonging to 14 families. Various gastric lesions were confirmed in 15 patients (68.2 per cent) belonging to 13 familie... | [
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PMID:26634 | Morphologic aspects of bone marrow transplantation in patients with aplastic anemia. | Pre- and post-transplant bone marrow samples from 20 patients with aplastic anemia were studied. Morphologic evidence of marrow reconstitution was noted in 18 patients one to three weeks following transplantation. In most instances the engrafted marrow elements in early weeks appeared as small clusters of erythroid or ... | Morphologic aspects of bone marrow transplantation in patients with aplastic anemia. Pre- and post-transplant bone marrow samples from 20 patients with aplastic anemia were studied. Morphologic evidence of marrow reconstitution was noted in 18 patients one to three weeks following transplantation. In most instances the... | [
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PMID:26636 | Mice bearing the ob/ob mutation have impaired immunity. | The obese mutant mouse C57BL/6J ob/ob showed impaired ability to reject skin grafts or react to a contact-sensitising agent in comparison with littermate controls (either +/ob or +/+). Ability of spleen cells from mice bearing the ob/ob mutation to produce a graft-versus-host reaction in C57BL/6J X DBA/2J F1 hybrid mic... | Mice bearing the ob/ob mutation have impaired immunity. The obese mutant mouse C57BL/6J ob/ob showed impaired ability to reject skin grafts or react to a contact-sensitising agent in comparison with littermate controls (either +/ob or +/+). Ability of spleen cells from mice bearing the ob/ob mutation to produce a graft... | [
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