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5-羟色胺7(5-HT7)受体拮抗剂SB-269970对大鼠激素及体温应答5-羟色胺1A/7(5-HT1A/7)受体激动剂8-羟基二丙胺基四氢萘(8-OH-DPAT)的影响。

Effects of the 5-HT7 receptor antagonist SB-269970 on rat hormonal and temperature responses to the 5-HT1A/7 receptor agonist 8-OH-DPAT.

作者信息

Faure Céline, Mnie-Filali Ouissame, Scarna Hélène, Debonnel Guy, Haddjeri Nasser

机构信息

Laboratory of Neuropharmacology and Neurochemistry, Faculty of Pharmacy, University of Claude Bernard Lyon I, France.

出版信息

Neurosci Lett. 2006 Aug 14;404(1-2):122-6. doi: 10.1016/j.neulet.2006.05.023. Epub 2006 Jun 8.

DOI:10.1016/j.neulet.2006.05.023
PMID:16759802
Abstract

The physiological function of 5-HT(7) receptors is not yet fully determined. This study was designed to characterize the involvement of 5-HT(7) receptor in rat body temperature regulation and in adrenocorticotropic hormone (ACTH) and corticosterone secretion. In the first part of our study, acute administration of SB-269970 (0.1-1 mg/kg, i.p.), a potent and selective 5-HT(7) receptors antagonist, dose-dependently prevented 5-HT(1A/7) receptor agonist 8-OH-DPAT (0.1 mg/kg, s.c.)-induced hypothermia and when the 5-HT(1A) receptor antagonist WAY-100,635 was co-injected with SB-269970, a reduction of the latter hypothermia was obtained in an additive manner. In contrast, 1 mg/kg (i.p.) of SB-269970 failed to prevent 8-OH-DPAT (0.5 mg/kg, s.c.)-induced increase of ACTH and corticosterone plasma levels. In conclusion, the present results unveil an additive effect of both 5-HT(1A) and 5-HT(7) receptors in core body temperature regulation.

摘要

5-羟色胺(7)受体的生理功能尚未完全明确。本研究旨在明确5-羟色胺(7)受体在大鼠体温调节以及促肾上腺皮质激素(ACTH)和皮质酮分泌过程中的作用。在我们研究的第一部分中,强效选择性5-羟色胺(7)受体拮抗剂SB-269970(0.1 - 1毫克/千克,腹腔注射)的急性给药,剂量依赖性地阻止了5-羟色胺(1A/7)受体激动剂8-羟基二丙胺基四氢萘(8-OH-DPAT,0.1毫克/千克,皮下注射)诱导的体温过低,并且当5-羟色胺(1A)受体拮抗剂WAY-100,635与SB-269970共同注射时,后者导致的体温过低以相加的方式减轻。相比之下,1毫克/千克(腹腔注射)的SB-269970未能阻止8-OH-DPAT(0.5毫克/千克,皮下注射)诱导的ACTH和皮质酮血浆水平升高。总之,目前的结果揭示了5-羟色胺(1A)和5-羟色胺(7)受体在核心体温调节中的相加作用。

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