PD 176252 -: The first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist

被引：51

作者：

Ashwood, V ^{[1
]}

Brownhill, V ^{[1
]}

Higginbottom, M ^{[1
]}

Horwell, DC ^{[1
]}

Hughes, J ^{[1
]}

Lewthwaite, RA ^{[1
]}

McKnight, AT ^{[1
]}

Pinnock, RD ^{[1
]}

Pritchard, MC ^{[1
]}

Suman-Chauhan, N ^{[1
]}

Webb, C ^{[1
]}

Williams, SC ^{[1
]}

机构：

[1] Univ Cambridge, Parke Davis Neurosci Res Ctr, Cambridge CB2 2QB, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(98)00462-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this paper we describe the development of a novel series of non-peptide, "balanced" neuromedin-B preferring (BB1)/gastrin-releasing peptide preferring (BB2) receptor ligands as exemplified by PD 176252. PD 176252, which exhibits nanomolar affinity for both the BE, (K-i=0.15nM) and BB2 (K-i=1.0nM) receptors, has been demonstrated to be a competitive antagonist at these bombesin receptor subtypes. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2589 / 2594

页数：6

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