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ID: ALA1131372

Journal: Bioorg Med Chem Lett

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

Authors: Ashwood V, Brownhill V, Higginbottom M, Horwell DC, Hughes J, Lewthwaite RA, McKnight AT, Pinnock RD, Pritchard MC, Suman-Chauhan N, Webb C, Williams SC.

Abstract: 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 BB1 (Ki = 0.15 nM) and BB2 (Ki = 1.0 nM) receptors, has been demonstrated to be a competitive antagonist at these bombesin receptor subtypes.

CiteXplore: 9873586

DOI: 10.1016/s0960-894x(98)00462-4