Small molecule somatostatin receptor subtype-2 antagonists

被引：11

作者：

Hay, BA ^{[1
]}

Cole, BM ^{[1
]}

DiCapua, F ^{[1
]}

Kirk, GW ^{[1
]}

Murray, MC ^{[1
]}

Nardone, RA ^{[1
]}

Pelletier, DJ ^{[1
]}

Ricketts, AP ^{[1
]}

Robertson, AS ^{[1
]}

Siegel, TW ^{[1
]}

机构：

[1] Pfizer Inc, Groton Labs, Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)00568-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The first potent small molecule sst2 antagonists are reported. Altering known sst2 agonist molecules yielded compounds with high sst2 binding affinity and full antagonist activity. Compound 7a, for example, displaced somatostatin binding to the sst2 receptor with an IC50 = 2.9 nM and antagonized somatostatin action with an IC50 = 29 nM. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2731 / 2734

页数：4

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