PD 165929 - The first high affinity non-peptide neuromedin-B (NMB) receptor selective antagonist

被引：36

作者：

Eden, JM ^{[1
]}

Hall, MD ^{[1
]}

Higginbottom, M ^{[1
]}

Horwell, DC ^{[1
]}

Howson, W ^{[1
]}

Hughes, J ^{[1
]}

Jordan, RE ^{[1
]}

Lewthwaite, RA ^{[1
]}

Martin, K ^{[1
]}

McKnight, AT ^{[1
]}

OToole, JC ^{[1
]}

Pinnock, RD ^{[1
]}

Pritchard, MC ^{[1
]}

SumanChauhan, N ^{[1
]}

Williams, SC ^{[1
]}

机构：

[1] UNIV CAMBRIDGE,PARKE DAVIS NEUROSCI RES CTR,CAMBRIDGE CB2 2QB,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 21期

关键词：

D O I：

10.1016/0960-894X(96)00481-7

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 neuromedin-B (NMB) receptor ligands as exemplified by PD 165929. PD 165929, which exhibits nanomolar affinity for the NMB receptor (Ki=6.3nM), has been demonstrated to be a competitive antagonist at this receptor (appK(B)=7.6nM) and is selective over the corresponding gastrin-releasing peptide (GRP) receptor type (Ki>10000nM). Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2617 / 2622

页数：6

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