title: PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
abstract: 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.
authors.affiliation: Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.
authors.forename: V
authors.initials: V
authors.lastname: Ashwood
authors.forename: V
authors.initials: V
authors.lastname: Brownhill
authors.forename: M
authors.initials: M
authors.lastname: Higginbottom
authors.forename: D C
authors.initials: DC
authors.lastname: Horwell
authors.forename: J
authors.initials: J
authors.lastname: Hughes
authors.forename: R A
authors.initials: RA
authors.lastname: Lewthwaite
authors.forename: A T
authors.initials: AT
authors.lastname: McKnight
authors.forename: R D
authors.initials: RD
authors.lastname: Pinnock
authors.forename: M C
authors.initials: MC
authors.lastname: Pritchard
authors.forename: N
authors.initials: N
authors.lastname: Suman-Chauhan
authors.forename: C
authors.initials: C
authors.lastname: Webb
authors.forename: S C
authors.initials: SC
authors.lastname: Williams
mesh_terms: 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
chemical_list: D007211:Indoles; D008024:Ligands; C116775:PD 165929; D018004:Receptors, Bombesin; D019886:Gastrin-Releasing Peptide; D015287:Neurokinin B; C038393:neuromedin B; C116774:PD 176252