Design of novel cholecystokinin-B receptor ligands based on the 'double-ring system' approach.
A structurally novel series of cholecystokinin-B (CCK-B) receptor ligands has been designed and synthesized based on the 'double ring system' theory of receptor recognition. Compounds 2b-cis and 2g-cis from this 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 are discussed in the context of ongoing efforts to identify the CCK-B receptor binding site for nonpeptide ligands.
Lowe
J A
JA
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
Qian
W
W
McLean
S
S
Bryce
D K
DK
Crawford
R T
RT
Olsson
L C
LC
Bordner
J
J
D001665:Binding Sites; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D015195:Drug Design; D008958:Models, Molecular; D011487:Protein Conformation; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000737:chemistry / Q000378:metabolism*
D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin