Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists

被引：9

作者：

Daines, RA

Sham, KKC

Taggart, JJ

Kingsbury, WD

Chan, J

Breen, A

Disa, J

Aiyar, N

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT PHARMACOL,KING OF PRUSSIA,PA 19406

[2] SMITHKLINE BEECHAM PHARMACEUT,DEPT BIOMOL DISCOVERY,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10046-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A high-throughput screen identified quinine analog 1 as an antagonist of the human calcitonin gene-related peptide (hCGRP) receptor. Thus, compound 1 displaces [I-125]-CGRP from the hCGRP receptor and inhibits CGRP-mediated cAMP production with IC50 values of 5.9 +/- 1.2 mu M and 26 +/- 5 mu M, respectively. A limited structure-activity study of 1 is described. (C) 1997 Elsevier Science Ltd.

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页码：2673 / 2676

页数：4

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