Emicerfont (GW-876,008) is a drug developed by

GlaxoSmithKline GSK plc, formerly GlaxoSmithKline plc, is a British Multinational corporation, multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a Mergers and acquisitions, merger of Gl ...

which acts as a CRF-1 antagonist. Corticotropin releasing factor (CRF), also known as

Corticotropin releasing hormone Corticotropin-releasing hormone (CRH) (also known as corticotropin-releasing factor (CRF) or corticoliberin; corticotropin may also be spelled corticotrophin) is a peptide hormone involved in stress responses. It is a releasing hormone that bel ...

, is an endogenous peptide hormone which is released in response to various triggers such as

chronic stress Chronic stress is the physiological or psychological response induced by a long-term internal or external stressor. The stressor, either physically present or recollected, will produce the same effect and trigger a chronic stress response. There i ...

, and activates the two

corticotropin-releasing hormone receptor Corticotropin-releasing hormone receptors (CRHRs), also known as corticotropin-releasing factor receptors (CRFRs) are a G protein-coupled receptor family that binds corticotropin-releasing hormone (CRH). There are two receptors in the family, ...

s: CRF₁ and CRF₂. This then triggers the release of

corticotropin Adrenocorticotropic hormone (ACTH; also adrenocorticotropin, corticotropin) is a polypeptide tropic hormone produced by and secreted by the anterior pituitary gland. It is also used as a medication and diagnostic agent. ACTH is an important co ...

(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 Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain and or abdominal bloating and changes in the consistency of bowel movements. These symptoms ma ...

(IBS) and

alcoholism Alcoholism is, broadly, any drinking of alcohol that results in significant mental or physical health problems. Because there is disagreement on the definition of the word ''alcoholism'', it is not a recognized diagnostic entity. Predomina ...

, 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.

References

Corticotropin-releasing hormone antagonists Corticotropin-releasing hormone Imidazolidinones Phenol ethers Pyrrolopyridines {{systemic-hormonal-drug-stub

See also

References