PD-176252 - THE FIRST HIGH-AFFINITY NONPEPTIDE 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 SUMANCHAUHAN N WEBB C WILLIAMS SC
Citation
V. Ashwood et al., PD-176252 - THE FIRST HIGH-AFFINITY NONPEPTIDE GASTRIN-RELEASING PEPTIDE (BB2) RECEPTOR ANTAGONIST, Bioorganic & medicinal chemistry letters, 8(18), 1998, pp. 2589-2594
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
18
Year of publication
1998
Pages
2589 - 2594
Database
ISI
SICI code
0960-894X(1998)8:18<2589:P-TFHN>2.0.ZU;2-1
Abstract
In this paper we describe the development of a novel series of non-pep tide, ''balanced'' neuromedin-B preferring (BB1)/gastrin-releasing pep tide preferring (BB2) receptor ligands as exemplified by PD 176252. PD 176252, which exhibits nanomolar affinity for both the BE, (K-i=0.15n M) and BB2 (K-i=1.0nM) receptors, has been demonstrated to be a compet itive antagonist at these bombesin receptor subtypes. (C) 1998 Elsevie r Science Ltd. All rights reserved.