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Pexacerfont : ウィキペディア英語版
Pexacerfont

Pexacerfont (BMS-562,086) 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. 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, diabetes mellitus, osteoporosis, 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,〔(ClinicalTrials.gov: Study of Pexacerfont (BMS-562086) in the Treatment of Outpatients With Generalized Anxiety Disorder )〕 and has also been proposed to be useful for the treatment of depression and irritable bowel syndrome.〔(STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL )〕
A recent multicenter, randomized, double-blind, placebo-controlled trial found that Pexacerfont (100 mg/day) did not separate from placebo on the primary outcome measure (the mean change from baseline to end point in the Hamilton Anxiety Scale score). 〔Coric V, Feldman HH, Oren DA, Shekhar A, Pultz J, Dockens RC, Wu X, Gentile KA, Huang SP, Emison E, Delmonte T, D'Souza BB, Zimbroff DL, Grebb JA, Goddard AW, Stock EG (2010). Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder. Depress Anxiety. 27(5):417-25. PMID 20455246.〕 These results suggest that blockade of CRF-1 receptor may not be a feasible treatment for anxiety disorders in certain human populations.
== See also ==

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

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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