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]
^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. PMC3399687. 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. PMC3596012. 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. PMC4069031. PMID 23954313.
emicerfont, drug, developed, glaxosmithkline, which, acts, antagonist, corticotropin, releasing, factor, also, known, corticotropin, releasing, hormone, endogenous, peptide, hormone, which, released, response, various, triggers, such, chronic, stress, activate. 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 EmicerfontClinical dataRoutes ofadministrationOralATC codeNoneIdentifiersIUPAC name 1 1 1 4 methoxy 2 methylphenyl 6 methyl 2 3 dihydropyrrolo 2 3 b pyridin 4 yl pyrazol 3 yl imidazolidin 2 oneCAS Number786701 13 1PubChem CID11223423ChemSpider9398476UNIIOJ8EG4264PKEGGD09610CompTox Dashboard EPA DTXSID20229231Chemical and physical dataFormulaC 22H 24N 6O 2Molar mass404 474 g mol 13D model JSmol Interactive imageSMILES CC1 C C CC C1 OC N2CCC3 C2N C C C3N4C CC N4 N5CCNC5 O CEmicerfont 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 editCorticotropin releasing hormone antagonists Antalarmin Pexacerfont VerucerfontReferences edit 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 nbsp This hormonal preparation article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Emicerfont amp oldid 1157647070, wikipedia, wiki, book, books, library,
