5-羟色胺6受体在培养的纹状体神经元中与腺苷酸环化酶呈正向偶联。

5-HT6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture.

作者信息

Sebben M, Ansanay H, Bockaert J, Dumuis A

机构信息

CNRS UPR 9023, Mécanismes Moléculaires des Communications Cellulaires, C.C.I.P.E., Montpellier, France.

出版信息

Neuroreport. 1994 Dec 20;5(18):2553-7. doi: 10.1097/00001756-199412000-00037.

DOI:10.1097/00001756-199412000-00037

PMID:7696602

Abstract

5-HT receptor positively coupled to adenylyl cyclase in striatal neurones in culture does not correspond to the 5-HT4 receptor. 5-HT induces an increase in cAMP level with an EC50 of 125 nM. 5-HT agonists displayed the following rank order of potencies 5-HT > LSD > 5-MeOT > 5-CT. 8-OH-DPAT, RU 24969 and cisapride were inactive. The most efficacious antagonists were methiothepin and tricyclic antipsychotic drugs (clozapine, amitriptyline and nortryptyline). The pharmacological profile defined by both functional studies (cAMP level) and binding experiments ([125I]-LSD binding), and its localization in striatal neurones are in favour of the presence of the recently cloned 5-HT6 receptor in these cells.

摘要

培养的纹状体神经元中与腺苷酸环化酶正偶联的5-羟色胺（5-HT）受体并非5-HT4受体。5-HT诱导细胞内环磷酸腺苷（cAMP）水平升高，其半数有效浓度（EC50）为125纳摩尔。5-HT激动剂的效价顺序如下：5-HT＞麦角酰二乙胺（LSD）＞5-甲氧基色胺（5-MeOT）＞5-羧色胺（5-CT）。8-羟基二丙胺基四氢萘（8-OH-DPAT）、RU 24969和西沙必利无活性。最有效的拮抗剂是甲硫哒嗪和三环类抗精神病药物（氯氮平、阿米替林和去甲替林）。功能研究（cAMP水平）和结合实验（[125I]-LSD结合）所确定的药理学特征及其在纹状体神经元中的定位，均支持这些细胞中存在最近克隆出的5-HT6受体。