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[8-L-色氨酸]催产素的合成及其某些药理性质

Synthesis and some pharmacological properties of [8-L-tryptophan]oxytocin.

作者信息

Bodanszky M, Tolle J C, Seto J, Sawyer W H

出版信息

J Med Chem. 1980 Nov;23(11):1259-61. doi: 10.1021/jm00185a025.

Abstract

Condensation of (tert-butyloxycarbonyl)tocinoic acid with L-prolyl-L-tryptophylglycinamide produced the Boc derivative of a nonapeptide (disulfide) which on deprotection afforded [8-L-tryptophan]oxytocin. In assays on the rat uterus in vitro and in vivo the new analogue acts as both an agonist and an antagonist. The duration of both actions is prolonged.

摘要

(叔丁氧羰基)托西诺酸与L-脯氨酰-L-色氨酰甘氨酰胺缩合生成一种九肽(二硫键)的Boc衍生物,脱保护后得到[8-L-色氨酸]催产素。在大鼠子宫的体外和体内试验中,这种新类似物兼具激动剂和拮抗剂的作用。两种作用的持续时间都延长了。

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