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5-羟色胺和(+)-麦角酸二乙酰胺在大鼠边缘前脑的结合位点取代[3H]促甲状腺激素释放激素。

5-Hydroxytryptamine and (+)-lysergic acid diethylamide displace [3H]thyrotropin-releasing hormone at its binding sites in the rat limbic forebrain.

作者信息

Teshima S, Funatsu K, Satoh H, Inanaga K

出版信息

Regul Pept. 1986 Jul;14(4):293-9. doi: 10.1016/0167-0115(86)90171-0.

DOI:10.1016/0167-0115(86)90171-0
PMID:3018845
Abstract

Binding of [3H]thyrotropin-releasing hormone (TRH) to its receptors in the rat limbic forebrain was partially displaced by 5-hydroxytryptamine (5-HT, ligand for 5-HT1 receptors) and (+)-lysergic acid diethylamide ((+)-LSD, ligand for 5-HT1 and 5-HT2 receptors) at nanomolar concentrations. Spiperone (ligand for 5-HT2 receptors) displaced [3H]TRH in a dose-dependent manner at micromolar concentrations. These results suggest that some TRH receptors are related to 5-HT1 receptors, probably adjoining them on the membrane. This type of TRH receptor is shown to be among the high-affinity receptors which we reported previously. The significance of the receptor-coexistence is such that TRH facilitates serotonergic transmission by increasing the density of 5-HT1 receptors. This finding seems to support a pharmacological observation of other investigators that TRH potentiates 5-HT-induced hyperactivity in mice, probably by affecting postsynaptic 5-HT receptors.

摘要

[3H]促甲状腺激素释放激素(TRH)与大鼠边缘前脑受体的结合,在纳摩尔浓度下,被5-羟色胺(5-HT,5-HT1受体的配体)和(+)-麦角酸二乙胺((+)-LSD,5-HT1和5-HT2受体的配体)部分取代。螺哌隆(5-HT2受体的配体)在微摩尔浓度下以剂量依赖方式取代[3H]TRH。这些结果表明,一些TRH受体与5-HT1受体相关,可能在膜上与其相邻。这种类型的TRH受体被证明属于我们之前报道的高亲和力受体。受体共存的意义在于,TRH通过增加5-HT1受体的密度促进5-羟色胺能传递。这一发现似乎支持了其他研究者的药理学观察结果,即TRH可能通过影响突触后5-HT受体增强5-HT诱导的小鼠多动。

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