THE DEVELOPMENT OF A NOVEL SERIES OF NONPEPTIDE TACHYKININ NK3 RECEPTOR-SELECTIVE ANTAGONISTS

被引：25

作者：

BODEN, P ^{[1
]}

EDEN, JM ^{[1
]}

HODGSON, J ^{[1
]}

HORWELL, DC ^{[1
]}

PRITCHARD, MC ^{[1
]}

RAPHY, J ^{[1
]}

SUMANCHAUHAN, N ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 16期

关键词：

D O I：

10.1016/0960-894X(95)00313-I

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this paper we describe the transformation of a series of modified dipeptide NK3 receptor selective ligands, previously developed from a hit identified from the screening of a dipeptide chemical library, into non-peptide, nanomolar affinity NK3 receptor selective antagonists eg. PD160946 and PD161182. PD 161182 blocks senktide-induced human NK3 receptor mediated increases in intracellular calcium levels with a Ke of 0.88 nM.

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页码：1773 / 1778

页数：6

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