title: Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.
abstract: In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics properties and in vivo efficacy in rat models of gastric acid and pancreatic amylase secretion.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
authors.forename: Marna
authors.initials: M
authors.lastname: Pippel
authors.forename: Kristen
authors.initials: K
authors.lastname: Boyce
authors.forename: Hariharan
authors.initials: H
authors.lastname: Venkatesan
authors.forename: Victor K
authors.initials: VK
authors.lastname: Phuong
authors.forename: Wen
authors.initials: W
authors.lastname: Yan
authors.forename: Terrance D
authors.initials: TD
authors.lastname: Barrett
authors.forename: Guy
authors.initials: G
authors.lastname: Lagaud
authors.forename: Lina
authors.initials: L
authors.lastname: Li
authors.forename: Magda F
authors.initials: MF
authors.lastname: Morton
authors.forename: Clodagh
authors.initials: C
authors.lastname: Prendergast
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Wu
authors.forename: Nigel P
authors.initials: NP
authors.lastname: Shankley
authors.forename: Michael H
authors.initials: MH
authors.lastname: Rabinowitz
mesh_terms: D019943:Amino Acid Substitution; D000818:Animals; D007555:Isoxazoles / Q000737:chemistry*; D008958:Models, Molecular; D051381:Rats; D017208:Rats, Wistar; D043886:Receptor, Cholecystokinin A / Q000037:antagonists & inhibitors*; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000187:drug effects*; D013449:Sulfonamides / Q000494:pharmacology*; D016896:Treatment Outcome
chemical_list: D007555:Isoxazoles; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D013449:Sulfonamides; C033962:anthranil