蛙皮上皮细胞中5-羟色胺受体的药理学
Pharmacology of 5-hydroxytryptamine receptors in frog skin epithelium.
作者信息
Dalton T
出版信息
Br J Pharmacol. 1979 Apr;65(4):579-85. doi: 10.1111/j.1476-5381.1979.tb07867.x.
Abstract
- 5-Hydroxytryptamine (5-HT) stimulates active sodium transport and decreases the passive mucosal to serosal chloride permeability across frog skin. The relative importance of the different regions of the 5-HT molecule in the mediation of these responses has been studied using a range of structurally related compounds. 2. Substitution in the ethyl amine side chain of 5-HT (5-hydroxytryptophan) results in decreased receptor affinity and intrinsic activity; removal of the side chain (5-hydroxyindole) abolishes activity. Methoxy substitution of the 5-OH moiety of 5-HT has no effect on intrinsic activity but reduces affinity; displacement of the hydroxyl group to position 6 diminishes intrinsic activity and affinity. 3. It is concluded that both of the 5-HT-induced physiological effects are mediated via a single receptor which is distinct from alpha- and beta-adrenoceptors.
摘要
- 5-羟色胺（5-HT）刺激主动钠转运，并降低蛙皮黏膜到浆膜的被动氯化物通透性。使用一系列结构相关化合物研究了5-HT分子不同区域在介导这些反应中的相对重要性。2. 5-HT乙胺侧链（5-羟色氨酸）的取代导致受体亲和力和内在活性降低；侧链去除（5-羟吲哚）则消除活性。5-HT的5-OH基团的甲氧基取代对内在活性无影响，但降低亲和力；羟基位移到6位会降低内在活性和亲和力。3. 得出结论，5-HT诱导的两种生理效应均通过与α和β肾上腺素能受体不同的单一受体介导。
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