Pexacerfont

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Pexacerfont
Pexacerfont.svg
Systematic (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
Clinical data
Legal status Uncontrolled
Routes Oral
Identifiers
CAS number 459856-18-9
ATC code None
PubChem CID 9884366
ChemSpider 8060040
UNII LF1VBG4ZUK YesY
KEGG D10022 YesY
Chemical data
Formula C18H24N6O 
Mol. mass 340.4 g/mol
 YesY (what is this?)  (verify)

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.[1]

Pexacerfont is a recently developed CRF-1 antagonist which is currently in clinical trials for the treatment of anxiety disorders,[2] and has also been proposed to be useful for the treatment of depression and irritable bowel syndrome.[3]

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). [4] These results suggest that blockade of CRF-1 receptor may not be a feasible treatment for anxiety disorders in certain human populations.

See also[edit]

References[edit]

  1. ^ 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.
  2. ^ ClinicalTrials.gov: Study of Pexacerfont (BMS-562086) in the Treatment of Outpatients With Generalized Anxiety Disorder
  3. ^ STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL
  4. ^ 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.