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[关于普拉米维林的抗胆碱活性]

[On the cholinolytic activity of pramiverine].

作者信息

Enenkel H J, Müller-Calgan H, Schorscher E

出版信息

Arzneimittelforschung. 1976 Apr;26(4b):690-6.

PMID:821493
Abstract

Pharmacological experiments with the spasmolytic 4,4-diphenyl-N-isopropyl-cyclohexylamine hydrochloride (pramiverine, Sistalgin) are reported. The anticholinergic and spasmolytic action was tested in vitro on segments of abdominal organs in comparison with atropin, hyoscin-N-butylbromide and Eupaverin. Acetylcholine, arecoline, carbachol and pilocarpine were used as cholinergic agonists. Besides, neostigmine was applied. Pramiverine is distinguished by a strong anticholinergic and a papaverine-like spasmolytic component. In vitro the anticholinergic action of pramiverine on the small intestine (guinea pig, rabbit), gall bladder (guinea pig) and uterus (guinea pig, rat) was equally strong as the effect of atropine, but on the urinary bladder (guinea pig) the effect was 5 times weaker. The anticholinergic effect was also demonstrated in other models: intestinal spasms after neostigmine injection in the guinea pig; hypotensive effect after acetylcholine administration in rabbits, cats and dogs; salivation after pilocarpine administration in rabbits; tremorine test in rats. The gastric secretion in the Shay rat and the gastrointestinal passage were reduced or inhibited by pramiverine. The test substance was also active on oral application.

摘要

报道了用解痉药4,4-二苯基-N-异丙基环己胺盐酸盐(普拉米维林,西斯塔金)进行的药理实验。与阿托品、丁溴东莨菪碱和优帕韦林相比,在体外对腹部器官节段测试了其抗胆碱能和解痉作用。乙酰胆碱、槟榔碱、卡巴胆碱和毛果芸香碱用作胆碱能激动剂。此外,还应用了新斯的明。普拉米维林具有强烈的抗胆碱能和类似罂粟碱的解痉成分。在体外,普拉米维林对小肠(豚鼠、兔)、胆囊(豚鼠)和子宫(豚鼠、大鼠)的抗胆碱能作用与阿托品的作用同样强烈,但对膀胱(豚鼠)的作用弱5倍。在其他模型中也证实了其抗胆碱能作用:豚鼠注射新斯的明后的肠痉挛;兔、猫和狗注射乙酰胆碱后的降压作用;兔注射毛果芸香碱后的唾液分泌;大鼠的震颤素试验。普拉米维林可减少或抑制沙伊大鼠的胃酸分泌和胃肠道蠕动。该受试物质口服时也有活性。

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1
[On the cholinolytic activity of pramiverine].[关于普拉米维林的抗胆碱活性]
Arzneimittelforschung. 1976 Apr;26(4b):690-6.
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