L-708,474 - THE C5-CYCLOHEXYL ANALOG OF L-365,260, A SELECTIVE HIGH-AFFINITY LIGAND FOR THE CCK(B)/GASTRIN RECEPTOR

被引：27

作者：

CHAMBERS, MS

HOBBS, SC

FLETCHER, SR

MATASSA, VG

MITCHELL, PJ

WATT, AP

BAKER, R

FREEDMAN, SB

PATEL, S

SMITH, AJ

机构：

[1] Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex CM20 2QR, Terlings Park, Eastwick Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)80987-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The C5-cyclohexyl analogue of the cholecystokinin type-B (CCKB) receptor antagonist L-365,260 has been prepared. This derivative has significantly higher CCKB affinity and markedly improved CCKB/CCKA receptor selectivity (6,500 v. 87-fold) than the parent compound. It is one of the most potent and selective CCKB ligands reported to date.

引用

页码：1919 / 1924

页数：6

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