摘要:

The efficacy of the synthetic glucocorticoid, methylprednisolone, was examined in vitro using an isolated cat liver perfused with a blood-free medium. Addition of endotoxin (75 µg/g tissue) to the perfusate did not change perfusion pressure or total oxygen consumption. However, cellular integrity was severely compromised as reflected by increases in perfusate lactate dehydrogenase and cathepsin D activities, increases in tissue lysosomal fragility, and enlargement and vacuolization of lysosomes. Addition of methylprednisolone (1 x 10–3 M) to the perfusion medium prevented the endotoxin-induced changes in hepatocyte integrity. It is suggested that a major action of endotoxin in the liver is to increase lysosomal fragility, and the protective action of methylprednisolone appears to be related to its lysosomal stabilizing action. The potent anti-endotoxin action of glucocorticoids in vivo may be due in part to the stabilization of lysosomal membranes in tissues such as the liv

ISSN:0031-7012    

DOI:10.1159/000136853

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

The plasma elimination rates of phenacetin, acetanilide and theophylline have been determined in 32 healthy subjects in an effort to find drugs resembling in their metabolism the carcinogen benzo(a)pyrene. The plasma half-lives and metabolic clearance rates of the three drugs were correlated with the inducibilities of aryl hydrocarbon hydroxylase (AHH) in mitogen-stimulated lymphocytes and the plasma half-lives and metabolic clearance rates of antipyrine determined in previous studies. Statistically significant correlations were found between the half-lives and metabolic clearance rates of phenacetin, acetanilide and theophylline and the AHH ratios except for the metabolic clearance rates of phenacetin which did not correlate. The correlations of the three drugs with the half-lives and metabolic clearance rates of antipyrine were equally good. Of all the drugs tested thus far for similarity in metabolism to benzo(a)pyrene, antipyrine showed the best association followed closely by theophylline.

ISSN:0031-7012    

DOI:10.1159/000136854

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

Pretreatment of 3 male rhesus monkeys (Macaca muhtta) with SKF 525-A(20 mg/kg, i.m.) 3 h prior to injecting 14CH3-N-antipyrine (30 mg/kg, i.v.) increased antipyrine plasma half-life (APH) 240–500%; measurements of APH made 4, 8 and 11 days after SKF 525-A treatment were also higher than control values. Increases correspond to decreased plasma levels of 3-hydroxy-methylantipyrine and 4-hydroxyantipyrine and decreased rates of aldrin epoxidation in liver biopsy homogenates. Comparison of HSLC and radiometric methods for determining APH showed that both methods were capable of detecting chemically altered hepatic monooxygenase activit

ISSN:0031-7012    

DOI:10.1159/000136855

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

A putative neurotransmitter, 2-phenylethylamine, which is most highly concentrated in the extrapyramidal system of human brain, is able to reverse reserpine-induced parkinsonism in animals and elicit stereotypy. This action is only partially antagonized after catecholamine depletion by pretreatment with α-methyl-paratyrosine, and fully blocked by pretreatment with haloperidol, a dopamine receptor blocker. Therefore, via direct and/or indirect actions, 2-phenyl-ethylamine may serve a neuroregulatory role in the extrapyramidal system

ISSN:0031-7012    

DOI:10.1159/000136856

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

Kinetic parameters of morphine and azidomorphine derivatives as well as methionine enkephalin methylester were determined on the electrically stimulated isolated medial smooth muscle of the cat nictitating membrane. The organ was found to be a promising in vitro model for testing the action of opiate agonists on opiate B receptors.

ISSN:0031-7012    

DOI:10.1159/000136857

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

The hyperglycemic activities of epinephrine (EPI) and isoproterenol (ISO) in baboons correlated with their ability to increase plasma glucagon (IRG) levels relative to insulin (IRI). EPI inhibited IRI release and produced greater increases in plasma glucose and IRG than did ISO. ISO increased plasma IRI levels more than IRG. Infusion of somatostatin blocked IRG release and inhibited hyperglycemic responses to EPI by approximately 50%. These findings indicate that, as in man, IRG release contributes significantly to the hyperglycemic effects of catecholamines in baboons. The baboon thus appears to be a suitable model for predicting effects of drugs on glucose homeostasis in humans.

ISSN:0031-7012    

DOI:10.1159/000136858

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

Body weight gain and food and water consumption of female rats receiving daily methadone injections (5 mg/kg) intraperitoneally prior to mating and during gestation and lactation were studied. In contrast to saline-injected mothers, methadone-treated females had lower body weights throughout pregnancy, but gained weight during lactation; by postnatal day 21, both groups were of comparable body weight. No significant differences in food consumption throughout gestation or lactation were recorded. Total water consumption of methadone-treated rats was higher during the first 2 weeks of gestation and lactation, and lower during the 3rd week of lactation when compared to controls. These results demonstrate that methadone-treated rats have lower body weights throughout gestation and lactation, and that these weight deficits are not caused by insufficient food and water consumption.

ISSN:0031-7012    

DOI:10.1159/000136859

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

The interaction of acenocoumarin, coumachlor, phenprocoumon, and warfarin with human and bovine serum albumin was investigated by ultracentrifugation and circular dichroism measurements. Although all four drugs generate extrinsic Cotton effects when bound to human and bovine serum albumin, large differences in the signs and the intensities of the Cotton effects are observed. The differences in the induced Cotton effects suggest differential molecular binding mechanisms.

ISSN:0031-7012    

DOI:10.1159/000136860

出版商:S. Karger AG    

年代:1978

数据来源: Karger

ISSN:0031-7012    

DOI:10.1159/000136861

出版商:S. Karger AG    

年代:1978

数据来源: Karger

ISSN:0031-7012    

DOI:10.1159/000137088

出版商:S. Karger AG    

年代:1967

数据来源: Karger