SYNTHESIS AND BIOLOGICAL-ACTIVITY OF CCK PEPTIDES WITH ANTAGONIST ACTIVITY FOR CCK-A-RECEPTOR

被引：3

作者：

BOOMGAARDEN, M ^{[1
]}

HENKLEIN, P ^{[1
]}

MORGENSTERN, R ^{[1
]}

SOHR, R ^{[1
]}

OTT, T ^{[1
]}

MARTINEZ, J ^{[1
]}

机构：

[1] CNRS,INSERM,CTR PHARMACOL ENDOCRINOL,F-34094 MONTPELLIER,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 09期

关键词：

CHOLECYSTOKININ; ANTAGONISTS; CCK-A-RECEPTOR; GUINEA PIG ILEUM CONTRACTION; PEPTIDE SYNTHESIS;

D O I：

10.1016/0223-5234(92)90028-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a series of cholecystokinin analogues derived from the well-known antagonist Ge 410 (Suc-Tyr(SO3)-Met-Gly-Trp-Met-Asp-beta-phenethylamide) is reported. Replacements of L-Trp by D-Trp, Asp by Glu and Met by Nle were carried out and the resulting changes in biological activities investigated. All compounds synthesized were tested for their ability to inhibit CCK-induced contraction on isolated guinea pig ileum. SAR studies for these compounds are discussed.

引用

页码：955 / 959

页数：5

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