Verucerfont

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
Clinical data
Routes of
administration		Oral
ATC code
  • none
Identifiers
IUPAC name
  • 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
ECHA InfoCard100.158.110
Chemical and physical data
FormulaC22H26N6O2
Molar mass406.490 g·mol−1
3D model (JSmol)
SMILES
  • CC[C@@H](c1nc(no1)C)Nc2cc(nc3n2nc(c3c4ccc(cc4C)OC)C)C
InChI
  • 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 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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