Pexacerfont

Pexacerfont

drugbox
IUPAC_name = 8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N- [(1R)-1-methylpropyl] pyrazolo [1,5-a] -1,3,5-triazin-4-amine



width = 180
CAS_number = 459856-18-9
synonyms = Pexacerfont
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DrugBank =
C = 18 | H = 24 | N = 6 | O = 1
molecular_weight = 340.4 g/mol
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legal_status = Investigational New Drug
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Pexacerfont (BMS-562086) is a drug developed by Bristol-Myers Squibb which acts as a CRF-1 antagonist.

Corticotropin releasing factor (CRF), also known as Corticotropin releasing hormone, is an endogenous peptide hormone which is released in response to various triggers such as chronic stress and drug addiction. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive glucocorticoid release, stomach ulcers, anxiety, depression, and development of high blood pressure and consequent cardiovascular problems. [Zoumakis E, Rice KC, Gold PW, Chrousos GP. Potential uses of corticotropin-releasing hormone antagonists. "Annals of the New York Academy of Sciences". 2006 Nov;1083:239-51.]

Pexacerfont is a recently developed CRF-1 antagonist which is currently in clinical trials for the treatment of anxiety disorders, [http://www.leaddiscovery.co.uk/trials/321/] and has also been proposed to be useful for the treatment of depression and irritable bowel syndrome. [http://www.ama-assn.org/ama1/pub/upload/mm/365/pexacerfont.pdf]

ee also

* Antalarmin
* CP-154,526
* Corticotropin releasing hormone antagonists

References


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