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公认的选择性5-羟色胺-2拮抗剂可阻断脉络丛中的5-羟色胺5-HT-1c受体。

Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus.

作者信息

Sanders-Bush E, Breeding M

机构信息

Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee.

出版信息

J Pharmacol Exp Ther. 1988 Oct;247(1):169-73.

PMID:3139864
Abstract

The binding of [3H]mianserin to rat choroid plexus was characterized and compared with two other radioligands that label the 5-HT (serotonin)-1c receptor ([3H]mesulergine and [125I] lysergic acid diethylamide). [3H]Mianserin binding to a crude membrane preparation of choroid plexus from rat brain was rapid, saturable and of high affinity (Kd = 1 nM). The density of sites labeled by [3H]mianserin and [3H]mesulergine was equal. Furthermore, an excellent correlation was found between the potencies of drugs in competing for [3H]mianserin binding and for [125]lysergic acid diethylamide binding. Based on these data, it was concluded that [3H]mianserin labels the 5-HT-1c binding site. Using this ligand, the binding of the putative selective 5-HT-2 antagonist ritanserin to the 5-HT-1c site was evaluated. Ritanserin was a potent inhibitor of [3H]mianserin binding with a Ki value of 0.2 nM. Functional studies of 5-HT-stimulated phosphoinositide hydrolysis, the transmembrane signaling pathway for the 5-HT-1c receptor, showed that ritanserin blocks the effect of 5-HT and that it functions as a competitive antagonist of the 5-HT-1c receptor in intact choroid plexus. The potencies of ritanserin and several other drugs, including other 5-HT-2 antagonists, at the 5-HT-1c binding site correlated with their potencies at blocking 5-HT-stimulated phosphoinositide hydrolysis.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

对[3H]米安色林与大鼠脉络丛的结合进行了表征，并与另外两种标记5-羟色胺（5-HT）-1c受体的放射性配体（[3H]美舒麦角和[125I]麦角酸二乙胺）进行了比较。[3H]米安色林与大鼠脑脉络丛粗膜制剂的结合迅速、可饱和且具有高亲和力（解离常数Kd = 1 nM）。[3H]米安色林和[3H]美舒麦角标记的位点密度相等。此外，在竞争[3H]米安色林结合和[125I]麦角酸二乙胺结合的药物效力之间发现了极好的相关性。基于这些数据，得出结论：[3H]米安色林标记5-HT-1c结合位点。使用这种配体，评估了推定的选择性5-HT-2拮抗剂利坦色林与5-HT-1c位点的结合。利坦色林是[3H]米安色林结合的有效抑制剂，抑制常数Ki值为0.2 nM。对5-HT刺激的磷脂酰肌醇水解（5-HT-1c受体的跨膜信号传导途径）的功能研究表明，利坦色林可阻断5-HT的作用，并且在完整的脉络丛中作为5-HT-1c受体的竞争性拮抗剂发挥作用。利坦色林和其他几种药物（包括其他5-HT-2拮抗剂）在5-HT-1c结合位点的效力与其阻断5-HT刺激的磷脂酰肌醇水解的效力相关。（摘要截短于250字）

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Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor.
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