DESIGN OF NOVEL CHOLECYSTOKININ-B RECEPTOR LIGANDS BASED ON THE DOUBLE-RING SYSTEM APPROACH

Authors
LOWE JA QIAN WM MCLEAN S BRYCE DK CRAWFORD RT OLSSON LC BORDNER J
Citation
Ja. Lowe et al., DESIGN OF NOVEL CHOLECYSTOKININ-B RECEPTOR LIGANDS BASED ON THE DOUBLE-RING SYSTEM APPROACH, Regulatory peptides, 65(1), 1996, pp. 11-14
Citations number
13
Categorie Soggetti
Endocrynology & Metabolism",Physiology
Journal title
Regulatory peptides → ACNP
ISSN journal
01670115
Volume
65
Issue
1
Year of publication
1996
Pages
11 - 14
Database
ISI
SICI code
0167-0115(1996)65:1<11:DONCRL>2.0.ZU;2-7
Abstract
A structurally novel series of cholecystokinin-B (CCK-B) receptor liga nds has been designed and synthesized based on the 'double-ring system ' theory of receptor recognition. Compounds 2b-cis and 2g-cis from thi s 1-amino-2-benzyltetralin series show modest CCK-B receptor affinity, with IC50 values of 48.5 nM and 39.0 nM, respectively. The results ar e discussed in the context of ongoing efforts to identify the CCK-B re ceptor binding site for nonpeptide ligands.