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大鼠海马体中的胆碱能终末拥有介导乙酰胆碱释放抑制作用的5-HT1B受体。

Cholinergic terminals in rat hippocampus possess 5-HT1B receptors mediating inhibition of acetylcholine release.

作者信息

Maura G, Raiteri M

出版信息

Eur J Pharmacol. 1986 Oct 7;129(3):333-7. doi: 10.1016/0014-2999(86)90443-7.

DOI:10.1016/0014-2999(86)90443-7
PMID:3780847
Abstract

The effects of 5-hydroxytryptamine (5-HT) on the release of [3H]acetylcholine ([3H]ACh) from rat hippocampal nerve endings were investigated using synaptosomes labelled with [3H]choline and depolarized in superfusion with 15 mM KCl. The release of [3H]ACh was concentration dependently inhibited by exogenous 5-HT. The concentration-response curve of 5-HT was shifted to the right in a parallel way by methiothepin. The 5-HT2 antagonists ketanserin or methysergide did not antagonize the effect of 5-HT. The 5-HT1 agonist 5-methoxy-3-[1,2,3,6-tetrahydropyridin-4-yl]-1H-indole (RU 24969) mimicked 5-HT, whereas the 5-HT1A selective agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) was ineffective. When used as a 5-HT1A/5-HT1B antagonist, (-)propranolol antagonized 5-HT whereas spiperone (a 5-HT1A displacer) did not. The 5-HT1C selective antagonist mesulergine was also ineffective towards 5-HT. It can be concluded that hippocampal cholinergic terminals are endowed with inhibitory 5-HT receptors which appear to belong to the 5-HT1B subtype.

摘要

利用用[³H]胆碱标记并在含15 mM氯化钾的灌注液中去极化的突触体,研究了5-羟色胺(5-HT)对大鼠海马神经末梢释放[³H]乙酰胆碱([³H]ACh)的影响。外源性5-HT对[³H]ACh的释放有浓度依赖性抑制作用。美噻吨使5-HT的浓度-反应曲线平行右移。5-HT₂拮抗剂酮色林或甲基麦角新碱不能拮抗5-HT的作用。5-HT₁激动剂5-甲氧基-3-[1,2,3,6-四氢吡啶-4-基]-1H-吲哚(RU 24969)模拟5-HT的作用,而5-HT₁A选择性激动剂8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)则无效。当用作5-HT₁A/5-HT₁B拮抗剂时,(-)普萘洛尔能拮抗5-HT,而螺哌隆(一种5-HT₁A置换剂)则不能。5-HT₁C选择性拮抗剂美舒麦角对5-HT也无效。可以得出结论,海马胆碱能终末具有抑制性5-HT受体,这些受体似乎属于5-HT₁B亚型。

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