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豚鼠盲肠带中两种明显不同的毒蕈碱型胆碱能受体机制。

Two apparently distinct muscarinic cholinoceptor mechanisms in guinea-pig taenia caecum.

作者信息

Hisayama T, Kumagai N, Takayanagi I

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.

出版信息

Jpn J Pharmacol. 1988 Apr;46(4):414-7. doi: 10.1254/jjp.46.414.

Abstract

Thirty-min treatment of guinea-pig taenia caecum with 300 nM propyl-benzilylcholine mustard (PrBCM) shifted the concentration-response curve for carbachol to the right with a reduction of the maximum contraction, but 90-min treatment did not result in further inhibition. Under these conditions, pilocarpine hardly contracted the preparations, and it competitively antagonized carbachol. Muscarinic agonists might interact with two types of receptor mechanisms and carbachol elicited a stimulus from both types, whereas pilocarpine did so predominantly from the PrBCM-sensitive one.

摘要

用300 nM丙基苄基胆碱氮芥(PrBCM)对豚鼠盲肠带进行30分钟处理,可使卡巴胆碱的浓度-反应曲线右移,最大收缩力降低,但90分钟处理并未导致进一步抑制。在这些条件下,毛果芸香碱几乎不使制剂收缩,且它对卡巴胆碱具有竞争性拮抗作用。毒蕈碱激动剂可能与两种受体机制相互作用,卡巴胆碱从两种机制均引发刺激,而毛果芸香碱主要从对PrBCM敏感的机制引发刺激。

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