title: Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.
abstract: A series of high affinity CRF receptor ligands with an imidazo[4,5-c]pyridine core is described. Individual analogues were synthesized and tested in vitro in rat brain receptors to determine binding affinity. The best compound was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po.
authors.affiliation: Discovery Chemistry-Wilmington, Bristol-Myers Squibb Company, Experimental Station, DE 19880, USA. argyrios.arvanitis@bms.com
authors.forename: Argyrios G
authors.initials: AG
authors.lastname: Arvanitis
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Rescinito
authors.forename: Charles R
authors.initials: CR
authors.lastname: Arnold
authors.forename: Richard G
authors.initials: RG
authors.lastname: Wilde
authors.forename: Lawrence W
authors.initials: LW
authors.lastname: Fitzgerald
authors.forename: Robert
authors.initials: R
authors.lastname: Zaczek
authors.forename: Paul R
authors.initials: PR
authors.lastname: Hartig
authors.forename: Scott
authors.initials: S
authors.lastname: Grossman
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Arneric
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: Richard E
authors.initials: RE
authors.lastname: Olson
authors.forename: David W
authors.initials: DW
authors.lastname: Robertson
mesh_terms: D000284:Administration, Oral; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D001008:Anxiety Disorders / Q000188:drug therapy; D001682:Biological Availability; D004285:Dogs; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D014151:Anti-Anxiety Agents; D008024:Ligands; D011725:Pyridines; D018019:Receptors, Corticotropin-Releasing Hormone