PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
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.
Ashwood
V
V
Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.
Brownhill
V
V
Higginbottom
M
M
Horwell
D C
DC
Hughes
J
J
Lewthwaite
R A
RA
McKnight
A T
AT
Pinnock
R D
RD
Pritchard
M C
MC
Suman-Chauhan
N
N
Webb
C
C
Williams
S C
SC
D000818:Animals; D019886:Gastrin-Releasing Peptide / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000378:metabolism*; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D015287:Neurokinin B / Q000031:analogs & derivatives / Q000378:metabolism; D051381:Rats; D018004:Receptors, Bombesin / Q000037:antagonists & inhibitors*; D013045:Species Specificity; D013329:Structure-Activity Relationship
D007211:Indoles; D008024:Ligands; C116775:PD 165929; D018004:Receptors, Bombesin; D019886:Gastrin-Releasing Peptide; D015287:Neurokinin B; C038393:neuromedin B; C116774:PD 176252