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Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.

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

Author information

1
Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.

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.

PMID:
9873586
DOI:
10.1016/s0960-894x(98)00462-4
[Indexed for MEDLINE]

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