The endogenous cerebral tetrapeptide 5-HT-moduline reduces in vivo the functional activity of central 5-HT1B receptors in the rat

被引：22

作者：

Seguin, L ^{[1
]}

Seznec, JC ^{[1
]}

Fillion, G ^{[1
]}

机构：

[1] INST PASTEUR,UNITE PHARMACOL NEUROIMMUNOENDOCRINIENNE,F-75724 PARIS 15,FRANCE

来源：

NEUROSCIENCE RESEARCH | 1997年 / 27卷 / 03期

关键词：

5-HT1B receptors; adenylyl cyclase activity; 5-HT-moduline; desensitization; rat;

D O I：

10.1016/S0168-0102(96)01150-9

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

5-HT-moduline (Leu-Ser-Ala-Leu, LSAL) is a novel endogenous peptide isolated from rat brain which, interacts in vitro specifically with 5-HT1B receptors by a non-competitive mechanism. In the present study, we demonstrate that the efficacy of the selective 5-HT1B receptor agonist CP 93129 in inhibiting the forskolin-stimulated adenylyl cyclase activity in the rat substantia nigra was reduced 15 min after intracerebral injection of LSAL compared to vehicle or ALLS (scrambled peptide) injected rats. Accordingly, the concentration-response curve of the agonist is shifted to the right with a 3.5-fold increase of the half-maximal inhibitory concentration compared to vehicle injected rats. Thus, the in vivo desensitization of serotonergic autoreceptors strongly strengthens the important role of 5-HT-moduline in the rapid adaptative control of the serotonergic system, implicated in numerous pathological events as anxiety and depression. (C) 1997 Elsevier Science Ireland Ltd.

引用

页码：277 / 280

页数：4

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