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血清素通过5-HT3受体提高神经元细胞系中的环鸟苷酸水平。

Serotonin raises the cyclic GMP level in a neuronal cell line via 5-HT3 receptors.

作者信息

Reiser G, Hamprecht B

机构信息

Physiologisch-chemisches Institut, Universität Tübingen, F.R.G.

出版信息

Eur J Pharmacol. 1989 May 11;172(2):195-8. doi: 10.1016/0922-4106(89)90010-2.

Abstract

Serotonin (5-HT) induced a transient rise of the cyclic GMP level in neuroblastoma X glioma hybrid cells, half-maximally at 1 microM 5-HT. 2-Methyl-5-HT displayed an about 5 times lower potency but equal efficacy. alpha-Methyl-5-HT and 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) were completely ineffective at concentrations up to 30 microM. Antagonists specific for 5-HT3 receptors, ICS 205-930, GR 38032 F and MDL 72222, blocked the response to 5-HT at nanomolar concentrations but antagonists directed towards 5-HT1 and 5-HT2 receptors, ketanserin and methysergide, had no effect at concentrations up to 1 microM. Thus, 5-HT3 receptors are responsible for activating guanylate cyclase in the hybrid cells.

摘要

血清素(5-羟色胺,5-HT)可使神经母细胞瘤X胶质瘤杂交细胞中的环磷酸鸟苷(cGMP)水平短暂升高,在1微摩尔5-HT时达到最大效应的一半。2-甲基-5-HT的效力约低5倍,但效能相同。α-甲基-5-HT和8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)在浓度高达30微摩尔时完全无效。对5-HT3受体具有特异性的拮抗剂ICS 205-930、GR 38032 F和MDL 72222在纳摩尔浓度下可阻断对5-HT的反应,但针对5-HT1和5-HT2受体的拮抗剂酮色林和麦角新碱在浓度高达1微摩尔时无作用。因此,5-HT3受体负责激活杂交细胞中的鸟苷酸环化酶。

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