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PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. 1998
V Ashwood, and
V Brownhill, and
M Higginbottom, and
D C Horwell, and
J Hughes, and
R A Lewthwaite, and
A T McKnight, and
R D Pinnock, and
M C Pritchard, and
N Suman-Chauhan, and
C Webb, and
S C Williams
Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.
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.
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