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[丁螺环酮样5-羟色胺激动剂抗精神病作用的可能神经化学机制]

[The possible neurochemical mechanisms of the neuroleptic action of buspirone-like serotonin agonists].

作者信息

Kharin N A, Dolzhenko A T, Titievskiĭ A V, Naletov S V

出版信息

Eksp Klin Farmakol. 1993 Jul-Aug;56(4):12-4.

PMID:8106056
Abstract

The experiments on animals (rats and mice) and pigeons have established that buspirone and other serotonin agonists such as 1-(2-pyrimidinyl)-piperazine derivatives such as ipsapirone (TVX Q 7821), levopirone, kampirone, and sepirone have some pharmacological properties which are typical of neuroleptics. The serotonin agonists under study accelerate rat brain dopamine metabolism show their antagonism with apomorphine in the stereotypy and climbing tests in mice, suppress the conditioned avoidance reflex in rats, and eliminate apomorphine-induced vomiting in pigeons. Serotonin agonists, like serotonin, have been shown to stimulate the impulse-dependent release of 3H-dopamine from the slices of the rat nucleus accumbens and striatum. The capacity of buspirone and other serotonin antagonists of modulating dopamine release is not eliminated by 1A/B and 2 serotonin antagonists such as propranolol (3 microM) and metesergide (1 microM), but it is inhibited by ICS 205-930, a selective antagonist of 3HT receptors.

摘要

在动物(大鼠和小鼠)及鸽子身上进行的实验已证实,丁螺环酮和其他血清素激动剂,如1-(2-嘧啶基)-哌嗪衍生物,如伊沙匹隆(TVX Q 7821)、左匹隆、坎匹隆和塞匹隆,具有一些典型的抗精神病药物的药理特性。所研究的血清素激动剂能加速大鼠脑内多巴胺代谢,在小鼠的刻板行为和攀爬试验中显示出与阿扑吗啡的拮抗作用,抑制大鼠的条件性回避反射,并消除鸽子中阿扑吗啡引起的呕吐。血清素激动剂与血清素一样,已被证明能刺激大鼠伏隔核和纹状体切片中依赖冲动释放的3H-多巴胺。丁螺环酮和其他血清素拮抗剂调节多巴胺释放的能力不会被1A/B和2类血清素拮抗剂如普萘洛尔(3 microM)和美西麦角(1 microM)消除,但会被3HT受体的选择性拮抗剂ICS 205-930抑制。

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