title: Corticotropin-releasing factor antagonists: recent advances and exciting prospects for the treatment of human diseases.
abstract: Corticotropin-releasing factor (CRF) co-ordinates the neural, endocrine and immune responses of the body to stress. Several studies have implicated CRF in the etiology of anxiety, depression, substance abuse, stress-related gastrointestinal disorders and preterm labor, and intensive research into the design of safe and effective CRF antagonists is currently being pursued in several laboratories. Recently, improvements have been made not only in brain penetrance and in vivo activity in preclinical models for anxiety, depression and irritable bowel syndrome, but also in structural diversity for these compounds. Clinical data for R-121919 (NBI-30775; Neurocrine Biosciences Inc) raises the expectation that safe and potent CRF antagonists might be useful as drugs for the treatment of human diseases.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Neuroscience Chemistry, 5 Research Parkway, Wallingford, CT 06492, USA. paul.j.gilligan@bms.com
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: Yu-Wen
authors.initials: YW
authors.lastname: Li
mesh_terms: D000818:Animals; D003346:Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors* / Q000502:physiology / Q000627:therapeutic use*; D005544:Forecasting; D006801:Humans; D008024:Ligands; D008722:Methods; D015394:Molecular Structure; D018019:Receptors, Corticotropin-Releasing Hormone / Q000187:drug effects / Q000502:physiology; D013997:Time Factors
chemical_list: D008024:Ligands; D018019:Receptors, Corticotropin-Releasing Hormone; D003346:Corticotropin-Releasing Hormone