Emicerfont

Emicerfont

Emicerfont
Systematic (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
Clinical data
Routes of
administration
Oral
Identifiers
CAS Registry Number
ATC code None
PubChem CID:
Chemical data
Formula C22H24N6O2
Molecular mass 404.465 g/mol

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 CRH-1 and CRH-2. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress.

Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release. It has been investigated for the treatment of irritable bowel syndrome 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, Kelleher DL, Tillisch K, Naliboff BD, Mayer EA. Corticotropin-releasing factor receptor 1 antagonist alters regional activation and effective connectivity in an emotional-arousal circuit during expectation of abdominal pain. J Neurosci. 2011 Aug 31;31(35):12491-500. doi: 10.1523/JNEUROSCI.1860-11.2011 PMID 21880911
  2. ^ Zorrilla EP, Heilig M, de Wit H, Shaham Y. Behavioral, biological, and chemical perspectives on targeting CRF(1) receptor antagonists to treat alcoholism. Drug Alcohol Depend. 2013 Mar 1;128(3):175-86. doi: 10.1016/j.drugalcdep.2012.12.017 PMID 23294766
  3. ^ Labus JS, Hubbard CS, Bueller J, Ebrat B, Tillisch K, Chen M, Stains J, Dukes GE, Kelleher DL, Naliboff BD, Fanselow M, Mayer EA. Impaired emotional learning and involvement of the corticotropin-releasing factor signaling system in patients with irritable bowel syndrome. Gastroenterology. 2013 Dec;145(6):1253-61.e1-3. doi: 10.1053/j.gastro.2013.08.016 PMID 23954313