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胆囊收缩素C末端七肽和八肽的2-苯乙酯及2-苯乙酰胺衍生物类似物。

2-Phenylethyl ester and 2-phenylethyl amide derivative analogues of the C-terminal hepta- and octapeptide of cholecystokinin.

作者信息

Fulcrand P, Rodriguez M, Galas M C, Lignon M F, Laur J, Aumelas A, Martinez J

机构信息

CNRS-INSERM Centre for Pharmacology and Endocrinology, Montpellier, France.

出版信息

Int J Pept Protein Res. 1988 Nov;32(5):384-95. doi: 10.1111/j.1399-3011.1988.tb01273.x.

Abstract

Syntheses of analogues of the C-terminal octa- and heptapeptide of cholecystokinin are described. These analogues were obtained by replacing the C-terminal phenylalanine residue by 2-phenylethyl alcohol or by 2-phenylethylamine derivatives and by replacing the tryptophan residue by a D-tryptophan. The CCK-derivatives were tested for their ability to inhibit binding of labeled CCK-8 to rat pancreatic acini and to guinea pig brain membranes, and for their action on stimulation of amylase release from rat pancreatic acini. Some of these derivatives appeared to exhibit only part of the CCK-activity on amylase release, the D-Trp analogues behaving as CCK-antagonists.

摘要

本文描述了胆囊收缩素C末端八肽和七肽类似物的合成。这些类似物是通过用2-苯乙醇或2-苯乙胺衍生物取代C末端苯丙氨酸残基,并用D-色氨酸取代色氨酸残基而获得的。对这些CCK衍生物进行了测试,以检测它们抑制标记的CCK-8与大鼠胰腺腺泡和豚鼠脑膜结合的能力,以及它们对刺激大鼠胰腺腺泡淀粉酶释放的作用。其中一些衍生物似乎仅表现出部分CCK对淀粉酶释放的活性,D-色氨酸类似物表现为CCK拮抗剂。

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