Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.
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.
Arvanitis
Argyrios G
AG
Discovery Chemistry-Wilmington, Bristol-Myers Squibb Company, Experimental Station, DE 19880, USA. argyrios.arvanitis@bms.com
Rescinito
Joseph T
JT
Arnold
Charles R
CR
Wilde
Richard G
RG
Fitzgerald
Lawrence W
LW
Zaczek
Robert
R
Hartig
Paul R
PR
Grossman
Scott
S
Arneric
Stephen P
SP
Gilligan
Paul J
PJ
Olson
Richard E
RE
Robertson
David W
DW
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
D014151:Anti-Anxiety Agents; D008024:Ligands; D011725:Pyridines; D018019:Receptors, Corticotropin-Releasing Hormone