摘要:

Abstract:Rats were given enibomal (60 mg/kg) intravenously in a single dose. Groups of animals were then killed after 15, 30, 60, 120, 180 and 240 min. respectively, and the concentrations of enibomal determined. In the plasma, liver and muscles the concentration was reduced between 15 and 30 minutes after the injection, after which it remained at a fairly constant level until one hour after the injection. The concentration then fell again in the plasma at a rate corresponding to a half‐value period of about 2 hours. In the brain a steep fall was seen during the first hour, after which the concentration fell at a slow rate. 15 minutes after the injection the concentration was nearly the same in the plasma and fatty tissue. Thereafter it rose steeply in the fat, to four times the value in the plasma within the first hour. Finally the fat concentration fell, to reach a level of about 40 per cent of the maximum value four hours after the injection. In urine of rats collected over 72 hours the following 5‐isopropylbarbituric acid derivates (B) were detected: l‐methyl‐5‐acetonyl‐B, 5‐acetonyl‐B, and l‐methyl‐5‐(2′‐oxo‐3′‐hydroxypropyl)‐B. About 20 per cent of the administered dose was recoverable in the urine. The kinds and amounts of metabolites were the same as previously found in human urine. Neither enimobal nor the metabolites were detectable in the bile or in the small‐intestinal contents within the f

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01486.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Commercial solutions of phenoxyacetic acids were tested for teratogenic effects in NMRI‐mice. The Swedish product Hormoslyr 500‐T contained only 2,4,5‐trichlorophenoxyacetic acid (2,4,5‐T) while Hormoslyr 64 was a mixture of 2,4‐dichlorophenoxyacetic acid (2,4‐D) and 2,4,5‐T (2:1). Subcutaneous injections were given from day 6 through day 14 of pregnancy and the animals were sacrificed on day 18. The number of resorbed embryos, living embryos with gross malformations, as well as internal and skeletal malformations were recorded. It was found that both preparations at the high dosage (110 mg/kg/day) were teratogenic and embryotoxic. At the low dose level (50 mg/kg/day) the 2,4,5‐T solution was more harmful than the mixture of 2,4‐D and 2,4,5‐T. The risks of teratogenicity in human civilian use and the role of di

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01487.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:It was found byin vitroexperiments that the protein binding of acetylsalicylic acid, salicylic acid, phenylbutazone, diphenylhydantoin, sulphadiazine and thiopental was decreased in the plasma of 10 surgical patients with acute renal failure. The plasma was taken 4 to 8 days after the onset of the renal failure. At a drug concentration of 400 μg/ml the decreases ranged from 21.8 to 60.3 % as compared with a normal control group. At drug concentrations in or near the normal therapeutic level, the protein binding was even more decreased for the salicylic acids and sulphadiazine but less decreased for diphenylhydantoin and thiopental. The decreased binding could only partly be explained by the lower concentration of albumin in the patients: 3.0 g/100 ml ± 0.48 (S.D.) compared to 4.1 g/100 ml ± 0.53 (S.D.) (P<0.0

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01488.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Mercaptodextran (SH‐dextran) proved to be less toxic than BAL in rodents and better tolerated in intravenous infusion therapy. Immediate therapy with SH‐dextran was superior to any other treatment for the removal of sublethal doses of mercury (1.8 μmol Hg/kg) from the body. The life‐saving effect of SH‐dextran given immediately after a lethal HgCl2‐dose (74 μmol Hg/kg) was demonstrated. When chelation therapy was given two hours after the poisoning, however, SH‐dextran was without any significant effect, while BAL was still life‐saving. Mercury mobilized from the kidneys was redistributed to other organs when immediate chelation treatment with low molecular thiols was given, whereas SH‐dextran brought about an excretion of mobilized mercury. SH‐dextran, in contrast to certain other antidotes, did not induce an increased deposition of m

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01489.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Administration to mice ofVespa orientalisvenom was found to cause acute tubular necrosis of the kidney. The proximal tubular epithelial cells showed an abundance of autophagic vacuoles, suggesting disintegration of mitochondria. A few necrotic cells were found. The mechanism of the action of the venom on the kidney tubule cells is as yet unknown but there is evidence for direct effect of the venom on the mitochondria.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01490.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Twentyfour patients with rheumatoid arthritis (A.R.A. criteria) were examined before and after a period of gold treatment (10–33 weeks). The Rheumatoid Activity Index (according to Lansbury1958) decreased significantly (mean ± S. D.: −33.2 ± 26, P<0.01) as did the tissue concentration of cortisol (skin biopsies at 8 a. m.). The values decreased on an average from 51 ng/g to 20 ng/g, the mean decrease ± S. D. being 33 ng/l ±55 (P<0.02). However, no significant correlation could be demonstrated between the fall in the Activity Index and the decrease in tissue cortisol. No consistent changes were found in the plasma cortisol (total or ultra‐filtrate). Similar to other non‐steroid anti‐inflammatory drugs, gold appears to exert a “non‐specific” influence on the distribution of

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01491.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The excretion of drugs in the tears of cattle was studied, while almost constant plasma concentrations were maintained by continuous intravenous infusion. The examination included both acid and basic drugs. A fairly constant ratio between the concentrations in the tears and the ultrafiltrate of plasma was found for each drug examined. The ratio was not influenced by the rate of secretion or the plasma concentration. For drugs of an acid nature the ratio was less than or equal to 1 (sulphanilamide 0.99, sulphadimidine 0.80, sulphadiazine 0.35, sulphadoxine 0.48, benzylpenicillin 0.004), whereas the ratio for drugs of a basic nature was greater than 1 (penethamate 7.1, trimethoprim 2.2). The above described investigations provide reasons for believing that the passage of the examined drugs from the plasma to the tears may take place by diffusion of the non‐protein‐bound, unionized fract

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01492.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:A method for experimental studyin vitroof the outlet region (bladder base, bladder neck and proximal urethra) from the cat is described which allows simultaneous recording of resistance to flow through the region and of isometric tension in the longitudinal muscles. The results suggest that acetylcholine (ACh) may influence the smooth muscles in the outlet region by several mechanisms. Contractions in the longitudinal muscles are mediated by atropine sensitive cholinergic receptors. The resistance to flow could be either increased or decreased following ACh stimulation and in neither case could the response be blocked with atropine. If the response was an increase, however, it was blocked by phentolamine and if it was a decrease, it was blocked by propranolol. It is concluded that ACh stimulates the circular musculature in the outflow region through α‐ and β‐adrenergic receptors. It is suggested that the effects of ACh on flow are brought about through short intramural adrenergic neurons. ACh stimulates their ganglion‐cells which results in a release of nor‐adrenaline at the nerve endings and in activation of adrenergic receptors in the circular mus

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01493.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Promazine and imipramine in concentrations between 0.005 mM and 0.20 mM, and thioridazine between 0.005 mM and 0.10 mM inhibitp‐amino‐phenol glucuronidation in rat hepatoma cell cultures. The cardiac stabilizers propranolol and quinidine have little or no effect on glucuronidation. In a homogenate system prepared from the cells promazine, thioridazine, and imipramine between 0.1 and 1.0 mM also inhibitp‐arninophenol glucuronidation. In addition, promazine, thioridazine, and imipramine inhibit alanine uptake/incorporation, α‐aminoisobutyric acid uptake and efflux in the cultures of hepato

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01494.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Guanethidine sulphate was administered intraperitoneally in a dose of 10‐60 mg/kg for up to two months to adult male rats and the content of guanethidine in the superior cervical ganglia was determined fluorometrically after combination with ninhydrin in alkaline solution. Guanethidine was shown to concentrate in the superior cervical ganglia. Twenty four hours after the discontinuation of guanethidine sulphate 20 mg/kg for 14 days, the mean total gang‐lionic content of guanethidine base was 50 ng/ganglion (S.D. 8.8, n = 10) corresponding to 83 μg/g dry weight or 17 μg/g wet weight. Following a single injection of guanethidine sulphate and following discontinuation of prolonged administration of the drug the ganglionic guanethidine declined with a half‐life of 35 hours. Most of the ganglia were excised 24 hours after discontinuation of administration of the drug at which time the decline in ganglionic guanethidine was exponential. Desmethylimipramine largely prevented the accumulation of guanethidine in the ganglia indicating a mainly intraneuronal localization of guanethidine, a localization which was confirmed by microautoradiography. Reserpine only lowered the content to a small extent possibly indicating a mainly extragranular localization of guanethidine in the nerve cells. The selective morphological effects of guanethidine on sympathetic ganglia previously demonstrated were almost completely prevented by desmethylimipramine but only to a small extent by reserpine. SKF‐525‐A potentiated the ganglionic effects of guanethidine. It is assumed that the ganglionic effects are due to a cytotoxic effect of guanethidine concentrating selectively in the sympathetic ganglion nerve cells with the major part being located outside the noradrenaline storage granules as opposed to a mainly intragranular localization in the peripheral sympatheti

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01495.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY