Verucerfont (GSK-561,679) is a drug developed by
GlaxoSmithKline 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 (biology), stress responses. It is a releasing ...
, 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 CRH-1 and CRH-2. 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 ...
(ACTH), another hormone which is involved in the physiological response to stress.
Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. It is under investigation as a potential treatment for
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. Predomi ...
, as chronic stress is often a factor in both development of alcoholism and relapse in recovering alcoholics. It has shown promising results in animal studies. However, human trials have shown that while the neuroendocrine effects translate from animal models, the alcohol anti-craving effects do not.
See also
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Antalarmin
Antalarmin (CP-156,181) is a drug that acts as a CRH1 antagonist.
Corticotropin-releasing hormone (CRH), also known as Corticotropin-releasing factor, is an endogenous peptide hormone released in response to various triggers such as chronic stres ...
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Corticotropin releasing hormone antagonists A Corticotropin-releasing hormone antagonist (CRH antagonist) is a specific type of receptor antagonist that blocks the receptor sites for corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF), which synchronizes the b ...
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List of investigational anxiolytics
This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in paren ...
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Pexacerfont
Pexacerfont (INN, previously known as BMS-562,086) is a drug developed by Bristol-Myers Squibb which acts as a CRF1 antagonist.
Corticotropin-releasing factor (CRF), also known as corticotropin-releasing hormone, is an endogenous peptide hormone ...
References
{{Reflist
Corticotropin-releasing hormone antagonists