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	786701-13-1;
PubChem CID	11223423;
ChemSpider	9398476;
UNII	OJ8EG4264P;
KEGG	D09610;
CompTox Dashboard (EPA)	DTXSID20229231 ;
Chemical and physical data
Formula	C22H24N6O2
Molar mass	404.474 g·mol−1
3D model (JSmol)	Interactive image;
	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]

References

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.
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.
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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[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.

Emicerfont

See also

References