摘要:

AbstractInjection of sublethal doses of soman in rat intraperitoneally or subcutaneously every 4, 8, 12 or 24 hours led to chronic LD50 doses which were markedly higher than the acute one. When rats were exposed every 24 hrs to half LD50 doses of soman, several of the animals did not show symptoms of soman poisoning and survived a total exposure of 4–7 times the acute LD50 dose. Brain and diaphragm acetylcholinesterase activities declined steadily during the chronic soman exposure. The so‐called external acetylcholinesterase activity of the diaphragm was inhibited to a slightly less degree than the total acetylcholinesterase of the same tissue. The ability of the liver to hydrolyze soman was similar in rats which survived several 24 hr doses and untreated r

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02411.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb03241.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb03242.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractFrom a homogenate of rabbit colon a crude protein kinase was isolated. The phosphorylation of histone by this enzyme was maximal at 20 mM NaF. Higher concentrations inhibited the incorporation of32P. After chromatography on a DEAE‐cellulose column the crude protein kinase was partly purified. Cyclic AMP and cGMP stimulated the protein kinases eluted at 0.09 M‐NaCl (Type I) and at ∼0.2M‐NaCl (Type II). The main peak was of type II. Mix (l‐methyl‐3‐isobutylxanthine) relaxed the rabbit colon muscle. The increase in the protein kinase activity was closely correlated to the changes of the cAMP level. The cGMP content was also increased. Isoprenaline increased the cAMP level and the protein kinase activity of the colon muscle. Isoprenaline had no effect on the cGMP level. It is suggested that relaxing drugs which increase the cAMP level of rabbit colon muscle may activate protein kinase. This enzyme might be an important factor of the cAMP mediated relax

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02412.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe possible calcium antagonistic action of the anti‐anginal drug terodiline was investigated by two experimental techniques. In isolated preparations of rabbit aorta and pregnant human uterus exposed to a calcium‐free medium and then depolarized by potassium, terodiline in concentrations of 4.5–36 μM inhibited contractions produced by cumulative addition of calcium to the extracellular medium. This effect of terodiline could be reversed by high concentrations of calcium. Within the same concentration range, terodiline also reduced potassium‐induced45Ca influx in isolated aorta without affecting calcium efflux. It is suggested that terodiline, which structurally has similarities to prenylamine and fendiline, like these drugs can be classified as a calcium an

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb03243.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe interaction of selenium with methyl mercury, methoxyethyl mercury and mercuric chloride was studied in a 37 days' experiment with rats. Liver, kidney, brain and faeces were analysed for mercury and selenium at the end of the experimental period. Selenium supplementation increased the retention of mercury in liver, when mercuric chloride was given, in liver and brain when methyl mercury was given, and in all tissues examined when methoxyethyl mercury was given. The Hg/Se molar ratios in the tissues have been calculated and are found to vary considerably.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02413.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe effects of terodiline on contractions induced in isolated rabbit detrusor by carbachol and potassium, and by electrical field stimulation were investigated. Terodiline relaxed preparations contracted by carbachol and potassium and, when added 15 min before stimulation, decreased the contractile responses to these agents in a concentration‐dependent way. Terodiline more effectively inhibited carbachol than potassium induced contractions. The “pure” calcium antagonist nifedipine had the opposite effect. Both atropine and terodiline caused a parallell shift to the right of the concentration‐response curve to carbachol. The maximum contractile tension and slope were not affected, suggesting a competitive antimuscarinic effect within the concentration range used. Atropine was approximately 750 times more potent than terodiline. The maximum inhibitory effect of atropine and the calcium antagonist nimodipine on the electrically induced response were 40 % and 69 %, respectively. Terodiline caused complete inhibition of the response, as also did a combination of nimodipine and atropine. — The results suggest that terodiline in low concentrations has mainly an antimuscarinic action. To this, a calcium antagonistic effect is added at higher concentrations. The two‐fold action of the drug makes it an effective inhibitor of bladder contraction, and an interesting tool for investigations of bladder co

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb03244.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractIn a 5 weeks' study rats were given mercuric, methoxyethyl mercury and methyl mercury alone or together with sodium selenite. The distribution of mercury and selenium among the soluble proteins of liver and kidneys has been investigated by gel chromatography. Estimates of the ratios of the concentration of mercury (selenium) of the soluble proteins to that of the precipitates of liver and kidney homogenates are reported. The ratios seem to decrease when selenium is given concomitant with mercury. When mercuric chloride was given alone, 50 per cent of the mercury content in the soluble kidney proteins was found in the fractions of proteins with a molecular weight similar to that of metallothionein. No mercury could be detected in these fractions when both mercuric chloride and sodium selenite were given.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02414.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractTerodiline, a drug with anticholinergic and calcium antagonistic properties, effectively relaxed carbachol‐contracted, isolated human bladder preparations. In the concentrations used, terodiline displaced to the right the concentration‐response curve obtained on cumulative addition of carbachol. The maximum response was slightly reduced only at the highest terodiline concentration used (5μM), suggesting a mainly competitive antimuscarinic effect. Nine patients, aged 12–78 years, suffering from urge urinary incontinence were investigated by simultaneous urethro‐cystometry before and after treatment with terodiline 12.5 mg twice or three times daily for 10 days. The patients reported subjective improvement with almost no side effects. Objectively, the number of uninhibited bladder contractions and the amplitude of the contractions decreased. The bladder capacity was almost doubled. There were no marked effects on bladder and urethral pressures at rest, and only two of the investigated patients had slight residual urine after treatment.The results suggest that terodiline is a promising alternative to existing drugs for inhibition of undesired detrusor

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb03245.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractAn inhalation exposure of male rats to 300 p.p.m. of a commercial turpentine 6 hrs daily 5 days a week for 8 weeks enhanced the activities of drug biotransformation enzymes of liver microsomes considerably. The activities of NADPH cytochromecreductase and 7‐ethoxycoumarin deethylase, and microsomal content of cytochrome P‐450 were increased 35–60 % during the first weeks of the experiment, but had a tendency to return towards the control values later on. A similar enhancement of activities was also found in liver microsomal epoxide hydratase and UDPglucuronosyltransferase, but these enzyme activities tended to adapt less during the experiment. The turpentine treatment increased the affinity of liver microsomal cytochrome P‐450 to α‐pinene (the main component of the turpentine). The present data suggests that exposure to turpentine is able to modify considerably the biotransformatio

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02415.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY