ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01533.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The toxicity of chlorpromazine (CPZ) and mescaline (MCL) to mouse cerebellum and fibroblast cells was studiedin vitro. CPZ proved to be more toxic than MCL to both tissues. Fibroblast celles are more sensitive than the cerebellum to both CPZ and MCL.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01534.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The effect of 150 mg/kg of L‐DOPA methylester on brain catecholamines was studied in adult and developing mice aged 3‐5 days and 13‐15 days. Noradrenaline was moderately increased in the developing brain but dopamine showed a manyfold increase. The increase of dopamine was less pronounced in adult brain. High doses of dl‐amphetamine (50‐160 mg/kg) injected to L‐DOPA pretreated mice further increased the dopamine levels in the developing brain. The adult brain catecholamines were remarkably depleted, provided the observation period was 4 hours after amphetamine. Amphetamine lowered the body temperature in mice aged 13‐15 days; the fall was dose‐dependent and potentiated by pretreatment with L‐DOPA. In adult mice amphetamine caused hyperthermia which was not modified by L‐DOPA. L‐DOPA did not change the mortality rates induced by amphetamine in developing mice, but infant mice pretreated with L‐DOPA showed a lower brain amphetamine concentration after death than the mice given amphetamine only. In adult mice GDOPA enhanced amphetamine toxicity. Special attention is paid to the importance of different turnover rates of catecholamines during development as well as to the complex action of amphetamine on enzymes regulating catecholamine turnover. It is assumed that the hypothermia of developing mice after amphetamine might result from the primary effect of amphetamine on

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01535.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Suspensions of rat intestinal cells were incubated for 30 min. at 38° with either sodium fluoride, sodium laurylsulphate or chlorhexidine acetate. Except for a slight stimulation with fluoride and laurylsulphate at the lowest concentration tested (0.05 mM), all three compounds progressively suppressed glucose utilization at increasing concentrations. A 50 % inhibition occurred at approximately 3 mM fluoride, 1 mM laurylsulphate and 0.2 mM chlorhexidine. Thus on an equimolar basis fluoride proved to be the least potent inhibitor of mucosal glucose metabolism. The implications of these findings are discussed with regard to the concentrations of these compounds used in oral therapeutics as well as to the amounts that may be swallowed and thereby reach the intestinal epithelium. According to the results from thisin vitrosystem, the amounts of fluoride tested are less likely to affect this essential digestive process than the corresponding quantities of laurylsulphate or chlorhexidine

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01536.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:Flupenthixol, a thioxanthene derivative may exist in two isomeric forms, α and β. Flupenthixol contains 45‐55 % α‐flupenthixol. The pharmacological effects of flupenthixol, α‐ and β‐flupenthixol have been compared with those of clopenthixol, chlorprothixene, fluphenazine, perphenazine, chlorpromazine and haloperidol. In most pharmacological screening tests α‐flupenthixol was equipotent with fluphenazine. β‐Flupenthixol showed very low pharmacological activity. As expected the potency of flupenthixol was about one half that of α‐flupenthixol. Flupenthixol was considerably more potent than clopenthixol and chlorprothixene in the inhibition of conditioned avoidance response. The influence on temperature regulation and the peripheral α‐adrenolytic effect was considerably weaker than

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01537.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The duration and intensity of the neuroleptic effect of α‐flupenthixol decanoate in viscoleo®have been compared with that of α‐flupenthixol, 2 HCl in aqueous solution and α‐flupenthixol base in viscoleo®in a number of animal experimental models. Incorporation of α‐flupenthixol base in oil led to a prolongation of the neuroleptic effect (apomorphine antagonism in dogs, inhibition of conditioned avoidance in rats and mice) as compared to the duration of the effect of α‐flupenthixol, 2 HCl in aqueous solution. In both cases marked sedation was observed. In contrast, there was no sedation after α‐flupenthixol decanoate in oil, but a slower, smoother onset and a much longer duration of neuroleptic effect resulted. In rats the cataleptic effect and the apomorphine antagonistic effect of α‐flupenthixol decanoate in oil were of much shorter duration than the inhibitory effect on conditioned avoidance response. In mice a slight potentiation of barbiturate anaesthesia could be demonstrated 1‐6 hrs after high doses of α‐flupenthixol decanoate in oil. The clinical advantages of the depo

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01538.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The characteristics of the interaction between dihydromorphine (DHM) and a synaptic plasma membrane (SPM) fraction from rat brain cerebral cortex have been studied. DHM at 10+9M concentration is bound in a reversible process which is partly specific. The specific binding is inhibited by the sulphydryl reagents, N‐ethylmaleimide andp‐chloromercuribenzoic acid. The binding is strongly inhibited by 10−8M levorphanol but significantly less inhibited by its optical antipode, dextrorphan, which is much less analgetic. At 10−8M concentration, nalorphine and naloxone were strongly inhibitory while heroin at 10−8M and codeine at 10−7M were nearly inactive. A mixture of 10−5M acetylcholine and 2.5 × 10−5M eserine caused a moderate inhibition while dopamine, noradrenaline, serotonin, histamine and propranolol were classified as inactive (i. e. caused less than 25 % inhibition at 10−5M). The observed binding characteristics of the SPM fraction are compatible with those which might be expected for the actual narcotic receptor. Analogous SPM preparations from subcortical parts of the cerebrum and from the brain stem also showed stereospecific bi

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01539.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The effect of noradrenaline antagonists, aceperone, phenoxybenzamine and dihydroergotamine and neuroleptic drugs with dopamine receptor blocking properties, i. e. haloperidol, perphenazine, trifluperazine, spiramide and pimozide was tested on the locomotor and rearing activity induced by amphetamine, 2.5 mg/kg, in rats. In general it was found that the neuroleptic drugs in very low doses, haloperidol, 0.10 mg/kg; perphenazine, 0.05 mg/kg; trifluperazine, 0.15 mg/kg; spiramide, 0.05 mg/kg and pimozide, 0.15 mg/kg produced complete inhibition of the amphetamine activities, whereas much higher doses of aceperone, 20 mg/kg and phenoxybenzamine, 20 mg/kg only produced partial antagonism. Dihydroergotamine (20 mg/kg) produced no significant effect on the amphetamine locomotor and rearing activity. In mice trifluperazine (0.2 and 0.4 mg/kg) produced a very marked inhibitory effect, whereas spiramide (0.15 and 0.20 mg/kg) produced a significant but short‐lasting effect on the locomotor activity after 4 and 8 mg/kg d‐amphetamine. Aceperone (5 and 10 mg/kg) and phenoxybenzamine (10 mg/kg) also produced a strong antagonistic effect on the motility. Furthermore α‐methyltyrosine (250 and 350 mg/kg), an inhibitor of the biosynthesis of dopamine and noradrenaline, produced complete inhibition, whereas FLA‐63 (20 and 40 mg/kg), an inhibitor of the formation of noradrenaline produced partial inhibition. In conclusion these results indicate that the locomotor effect in mice and rats after amphetamine is dependent on both dopaminergic and noradrenergic mechanisms. However, dopamine may be regarded as most significant, since the amphetamine motility only seems possible in the presence of functional active dopamine r

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01540.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:In African folk medicine an aqueous extract ofOldenlandia affinis DC, “Kalata‐Kalata”, is used to accelerate childbirth. From the extract, which induced strong contractions in isolated uteri, serotonin and an utero‐active polypeptide have been isolated. The peptide has been examined on oestrogen dominated uteri from rats and rabbitsin vivoandin vitroand also on human, uterine strips. The oxytocic activity showed the same threshold value of 20 üg/mlin vitrofor all three species.In vivothe same dose caused ventricular fibr

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01541.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY

摘要:

Abstract:The subcellular distribution and the latency of the lysosomal enzymes b‐glucuronidase and acid DNase have been studied in livers from ethanol treated and control rats. Some livers were isolated and perfused with or without ethanol. Ethanol treatment (4‐5 weeks) increased the free (non‐latent) lysosomal enzyme activity significantly without affecting the total activities. In the perfused liver ethanol produced a small stabilizing effect on the lysosomes. The lipid content of the liver did not change, and the plasma enzymes (alanine aminotransferase, aspartate arninotransferase, alkaline phosphatase, b‐glucuronidase) and plasma bilirubin were in the present study unaffected by the ethanol tr

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1973.tb01542.x

出版商:Blackwell Publishing Ltd    

年代:1973

数据来源: WILEY