5-羟色胺1A受体激动剂MKC-242可增加小鼠在高架十字迷宫中的探索活动。

The 5-HT1A receptor agonist MKC-242 increases the exploratory activity of mice in the elevated plus-maze.

作者信息

Sakaue Masaki, Ago Yukio, Sowa Chikako, Koyama Yutaka, Baba Akemichi, Matsuda Toshio

机构信息

Laboratory of Molecular Neuropharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, 565-0871, Osaka, Japan.

出版信息

Eur J Pharmacol. 2003 Jan 1;458(1-2):141-4. doi: 10.1016/s0014-2999(02)02786-3.

DOI:10.1016/s0014-2999(02)02786-3

PMID:12498918

Abstract

The effect of (S)-5-[3-[(1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxole HCl (MKC-242), a 5-HT(1A) receptor agonist, on mouse behavior was examined in the elevated plus-maze. MKC-242 significantly increased the percentage of open-arm entries and the percentage of open-arm time, indices of anxiety reduction, while it did not increase the enclosed-arm entries and time spent in enclosed arms. The effect of MKC-242 was antagonized by a low dose of the 5-HT(1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide which alone did not affect the behavior. These findings suggest that MKC-242 increases the exploratory activity of mice in the elevated plus-maze via activation of 5-HT(1A) receptors, probably the presynaptic autoreceptors.

摘要

在高架十字迷宫中检测了5-羟色胺（5-HT）1A受体激动剂（S）-5-[3-[(1,4-苯并二恶烷-2-基甲基)氨基]丙氧基]-1,3-苯并二恶烷盐酸盐（MKC-242）对小鼠行为的影响。MKC-242显著增加了进入开放臂的百分比和在开放臂停留的时间百分比，这是焦虑减轻的指标，而它并未增加进入封闭臂的次数和在封闭臂停留的时间。低剂量的5-HT1A受体拮抗剂N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-(2-吡啶基)环己烷甲酰胺可拮抗MKC-242的作用，该拮抗剂单独使用时不影响行为。这些发现表明，MKC-242通过激活5-HT1A受体（可能是突触前自身受体）增加小鼠在高架十字迷宫中的探索活动。