Verucerfont

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Verucerfont
Verucerfont structure.png
Systematic (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
Clinical data
Routes of
administration
Oral
Identifiers
CAS Number 885220-61-1
ATC code none
PubChem CID: 11596613
ChemSpider 28295024
UNII X60608B091 YesY
Chemical data
Formula C22H26N6O2
Molecular mass 406.480 g/mol
  • CC[C@@H](c1nc(no1)C)Nc2cc(nc3n2nc(c3c4cccc(c4C)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 but has not been tested in humans.[1]


See also

References

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  1. Zorrilla EP, Heilig M, de Wit H, Shaham Y. Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism. Drug and Alcohol Dependence. 2013 Mar 1;128(3):175-86. DOI 10.1016/j.drugalcdep.2012.12.017 PMID 23294766