Emicerfont Explained

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

• Corticotropin releasing hormone antagonists
  • Antalarmin
  • Pexacerfont
  • Verucerfont

Notes and References

1. Hubbard CS, Labus JS, Bueller J, Stains J, Suyenobu B, Dukes GE, Kelleher DL, Tillisch K, Naliboff BD, Mayer EA . 6 . 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 . August 2011 . 21880911 . 3399687 . 10.1523/JNEUROSCI.1860-11.2011 .
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 and Alcohol Dependence . 128 . 3 . 175–86 . March 2013 . 23294766 . 3596012 . 10.1016/j.drugalcdep.2012.12.017 .
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 . 6 . 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 . December 2013 . 23954313 . 4069031 . 10.1053/j.gastro.2013.08.016 .