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Pexacerfont
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
Identifiers
CAS number 459856-18-9
ATC code none
PubChem  ?
Chemical data
Formula C 18H24N6O 
Mol. mass 340.4 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Investigational New Drug
Routes  ?

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 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.[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]

See also

References

  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







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