拟抗精神病药去酪氨酸1-γ-内啡肽对体内3H-螺哌隆结合的抑制作用。

Inhibition of in vivo 3H-spiperone binding by the proposed antipsychotic Des-Tyr1-gamma-endorphin.

作者信息

Pedigo N W, Schallert T, Overstreet D H, Ling N C, Ragan P, Reisine T D, Yamamura H I

出版信息

Eur J Pharmacol. 1979 Dec 20;60(4):359-64. doi: 10.1016/0014-2999(79)90242-5.

Abstract

The proposed antipsychotic neuropeptide des-tyrosine1-gamma-endorphin (DT gamma E, beta LPH62,77) inhibits in vivo 3H-spiperone binding in the hypothalamus, corpus striatum and mesolimbic areas of rat brain. The neuroleptic drug haloperidol produces similar effects in these areas as well as in frontal cortex, but is considerably more potent than DT gamma E. Correspondingly, haloperidol produces postural and motor abnormalities not seen with DY gamma E. These data together with the results from previous in vitro studies suggest DT gamma E might act indirectly, having a selective neuroleptic-like action at 3H-spiperone binding sites.

摘要

所提出的抗精神病神经肽去酪氨酸1-γ-内啡肽（DTγE，β-LPH62,77）可抑制大鼠脑下丘脑、纹状体和中脑边缘区的体内3H-螺哌隆结合。抗精神病药物氟哌啶醇在这些区域以及额叶皮质也产生类似作用，但比DTγE的效力强得多。相应地，氟哌啶醇会产生DTγE未出现的姿势和运动异常。这些数据以及先前体外研究的结果表明，DTγE可能间接起作用，在3H-螺哌隆结合位点具有选择性的类抗精神病作用。