Verucerfont

Last updated

Verucerfont
Verucerfont.svg
Clinical data
Routes of
administration 		Oral
ATC code
  • none
Identifiers
  • 3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard 100.158.110 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C22H26N6O2
Molar mass 406.490 g·mol−1
3D model (JSmol)
  • CC[C@@H](c1nc(no1)C)Nc2cc(nc3n2nc(c3c4ccc(cc4C)OC)C)C
  • InChI=1S/C22H26N6O2/c1-7-17(22-24-15(5)27-30-22)25-19-11-12(2)23-21-20(14(4)26-28(19)21)16-9-8-10-18(29-6)13(16)3/h8-11,17,25H,7H2,1-6H3/t17-/m0/s1
  • Key:NZQAFTPOKINLRY-KRWDZBQOSA-N

Verucerfont (GSK-561,679) is a drug developed by GlaxoSmithKline 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 activates the two corticotropin-releasing hormone receptors CRH-1 and CRH-2. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress.

Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. It is under investigation as a potential treatment for alcoholism, as chronic stress is often a factor in both development of alcoholism and relapse in recovering alcoholics. It has shown promising results in animal studies. [1] However, human trials have shown that while the neuroendocrine effects translate from animal models, the alcohol anti-craving effects do not. [2]

See also

References

  1. ↑ Zorrilla EP, Heilig M, de Wit H, Shaham Y (March 2013). "Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism". Drug and Alcohol Dependence. 128 (3): 175–86. doi:10.1016/j.drugalcdep.2012.12.017. PMC   3596012 . PMID   23294766.
  2. ↑ Schwandt ML, Cortes CR, Kwako LE, et al. (April 2016). "The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects". Neuropsychopharmacology. 41 (12): 2818–2829. doi:10.1038/npp.2016.61. PMC   5061889 . PMID   27109623.
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