新型5-HT1A受体拮抗剂WAY 100635对离体中缝背核5-羟色胺能神经元和CA1锥体细胞的电生理效应
Electrophysiological effects of WAY 100635, a new 5-HT1A receptor antagonist, on dorsal raphe nucleus serotoninergic neurones and CA1 pyramidal cells in vitro.
作者信息
Corradetti R, Pugliese A M, Le Poul E, Laaris N, Hamon M, Lanfumey L
机构信息
Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy.
出版信息
Acta Physiol Hung. 1996;84(4):407-9.
The novel 5-HT1A receptor antagonist WAY 100635 [(N-(2-(-4(2-metoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyc lohexane carboxamide)] has been tested on 5-HT1A receptor-mediated inhibition of firing and intracellularly recorded hyperpolarisation of serotoninergic cells of the dorsal raphe nucleus (DRN) and on hyperpolarisation of hippocampal CA1 pyramidal cells. WAY 100635 selectively blocked 5-HT1A receptor-mediated responses of 5-HT, 8-OH-DPAT, lesopitron and 5-CT. The antagonism of the hyperpolarisation elicited by 5-CT was competitive in the DRN and non competitive in CA1, probably because of the existence of a 5-HT1A receptor reserve in serotoninergic cells of DRN.
新型5-羟色胺1A受体拮抗剂WAY 100635 [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]已针对5-羟色胺1A受体介导的放电抑制、背侧中缝核(DRN)5-羟色胺能细胞的细胞内记录超极化以及海马CA1锥体细胞的超极化进行了测试。WAY 100635选择性阻断5-羟色胺、8-羟基二丙胺基四氢萘、来索匹隆和5-羧色胺(5-CT)的5-羟色胺1A受体介导反应。5-CT引发的超极化拮抗作用在DRN中具有竞争性，而在CA1中无竞争性，这可能是由于DRN的5-羟色胺能细胞中存在5-羟色胺1A受体储备。
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