The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
1995; Elsevier BV; Volume: 5; Issue: 16 Linguagem: Inglês
10.1016/0960-894x(95)00313-i
ISSN1464-3405
AutoresP. Boden, J.M. Eden, Julie Hodgson, David C. Horwell, Martyn C. Pritchard, Jennifer Raphy, Nirmala Suman‐Chauhan,
Tópico(s)Pharmacological Receptor Mechanisms and Effects
ResumoIn 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 0.88nM.
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