Emicerfont

Emicerfont
Clinical data
Routes of
administration		Oral
ATC code
  • None
Identifiers
IUPAC name
  • 1-[1-[1-(4-methoxy-2-methylphenyl)-6-methyl-2,3-dihydropyrrolo[2,3-b]pyridin-4-yl]pyrazol-3-yl]imidazolidin-2-one
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H24N6O2
Molar mass404.474 g·mol−1
3D model (JSmol)
SMILES
  • CC1=C(C=CC(=C1)OC)N2CCC3=C2N=C(C=C3N4C=CC(=N4)N5CCNC5=O)C

Emicerfont (GW-876,008) 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: CRF1 and CRF2. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress.

Emicerfont blocks the CRF1 receptor, and so reduces ACTH release. It has been investigated for the treatment of irritable bowel syndrome (IBS) and alcoholism, and while it was not effective enough to be adopted for medical use in these applications, it continues to be used for research, as the role of the CRH-ACTH system in IBS remains poorly understood.[1][2][3]

See also

References

  1. ↑ Hubbard CS, Labus JS, Bueller J, Stains J, Suyenobu B, Dukes GE, et al. (August 2011). "Corticotropin-releasing factor receptor 1 antagonist alters regional activation and effective connectivity in an emotional-arousal circuit during expectation of abdominal pain". The Journal of Neuroscience. 31 (35): 12491–500. doi:10.1523/JNEUROSCI.1860-11.2011. PMC 3399687. PMID 21880911.
  2. ↑ 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.
  3. ↑ Labus JS, Hubbard CS, Bueller J, Ebrat B, Tillisch K, Chen M, et al. (December 2013). "Impaired emotional learning and involvement of the corticotropin-releasing factor signaling system in patients with irritable bowel syndrome". Gastroenterology. 145 (6): 1253–61.e1–3. doi:10.1053/j.gastro.2013.08.016. PMC 4069031. PMID 23954313.
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