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The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists

✍ Scribed by P. Boden; J.M. Eden; J. Hodgson; D.C. Horwell; M.C. Pritchard; J. Raphy; N. Suman-Chauhan

Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 222 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00313-i

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✦ Synopsis

In this paper we describe the transformation of a series of modified dipeptide NK 3 receptor selective ligands, previously developed from a hit identified from the screening of a dipeptide chemical library, into non-peptide, nanomolar affinity NK 3 receptor selective antagonists eg. PD160946 and PD161182. PD 161182 blocks senktideinduced human NK 3 receptor mediated increases in intracellular calcium levels with a Ke of 0.8gnM.

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