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促甲状腺激素释放激素(TRH):恢复小鼠中奥昔 tremorine 震颤。与5-羟色胺能和多巴胺能兴奋剂喹哌嗪的比较。

Thyrotropin releasing hormone (TRH): restoration of oxotremorine tremor in mice. Comparison with quipazine, a serotoninergic and dopaminergic stimulant.

作者信息

Kruse H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1976 Jul;294(1):39-45. doi: 10.1007/BF00692783.

Abstract

Both TRH and quipazine (2.5-25 mg/kg) were found to restore and to intensify the oxotremorine-induced tremor in mice when injected i.p. 60 min after oxotremorine 0.5 mg/kg s.c. This phenomenon does not seem to be due to an increase in body temperature or muscle tone. Also other dopaminergic drugs, e.g. amphetamine, methylphenidate, nomifensine and apomorphine had a significant but lesser effect than TRH or quipazine. Haloperidol and methysergide both antagonized the effect of quipazine but not that of TRH. Neither propranolol, phenoxybenzamine, alpha-methyl-p-tyrosine, nor p-chlorophenylalanine inhibited the activity of TRH or quipazine. The restoration of oxotremorine-induced tremor could be prevented by atropine but not by methylatropine. It is concluded that quipazine exerts its effect by direct stimulation of serotoninergic and dopaminergic receptors, whereas TRH receptors may represent separate entities and TRH may function as a neurotransmitter or neuromodulator.

摘要

当在皮下注射0.5mg/kg毒扁豆碱60分钟后腹腔注射时,发现促甲状腺激素释放激素(TRH)和喹哌嗪(2.5 - 25mg/kg)均可恢复并增强毒扁豆碱诱导的小鼠震颤。这种现象似乎不是由于体温或肌张力升高所致。其他多巴胺能药物,如苯丙胺、哌醋甲酯、诺米芬辛和阿扑吗啡也有显著作用,但比TRH或喹哌嗪的作用小。氟哌啶醇和麦角新碱均可拮抗喹哌嗪的作用,但不拮抗TRH的作用。普萘洛尔、酚苄明、α-甲基-对-酪氨酸或对氯苯丙氨酸均不抑制TRH或喹哌嗪的活性。阿托品可预防毒扁豆碱诱导的震颤恢复,而甲基阿托品则不能。结论是,喹哌嗪通过直接刺激5-羟色胺能和多巴胺能受体发挥作用,而TRH受体可能代表不同的实体,TRH可能作为神经递质或神经调节剂发挥作用。

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