Global InformationAntalarmin information
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| Other names | Antalarmin |
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| Formula | C24H34N4 |
| Molar mass | 378.564 g·mol−1 |
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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 stress and drug addiction. Such triggers result in the release of corticotropin (ACTH), another hormone involved in the physiological response to stress. Chronic release of CRH and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive glucocorticoid release, stomach ulcers, anxiety, diabetes mellitus, osteoporosis, depression, and development of high blood pressure and consequent cardiovascular problems.[1]
Antalarmin is a non-peptide drug that blocks the CRH1 receptor, and, as a consequence, reduces the release of ACTH in response to chronic stress.[2] This has been demonstrated in animals to reduce the behavioral responses to stressful situations,[3] and it is proposed that Antalarmin itself, or more likely newer CRH1 antagonist drugs still under development,[4] could be useful for reducing the adverse health consequences of chronic stress in humans, as well as having possible uses in the treatment of conditions such as anxiety, depression, and drug addiction.[5]
- ^ Zoumakis E, Rice KC, Gold PW, Chrousos GP (November 2006). "Potential uses of corticotropin-releasing hormone antagonists". Annals of the New York Academy of Sciences. 1083 (1): 239–51. Bibcode:2006NYASA1083..239Z. doi:10.1196/annals.1367.021. PMID 17148743. S2CID 7731338.
- ^ Webster EL, Lewis DB, Torpy DJ, Zachman EK, Rice KC, Chrousos GP (December 1996). "In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation". Endocrinology. 137 (12): 5747–50. doi:10.1210/endo.137.12.8940412. PMID 8940412.
- ^ Deak T, Nguyen KT, Ehrlich AL, Watkins LR, Spencer RL, Maier SF, et al. (January 1999). "The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress". Endocrinology. 140 (1): 79–86. doi:10.1210/endo.140.1.6415. PMID 9886810.
- ^ Nielsen DM, Carey GJ, Gold LH (September 2004). "Antidepressant-like activity of corticotropin-releasing factor type-1 receptor antagonists in mice". European Journal of Pharmacology. 499 (1–2): 135–46. doi:10.1016/j.ejphar.2004.07.091. PMID 15363960.
- ^ McCarthy JR, Heinrichs SC, Grigoriadis DE (May 1999). "Recent advances with the CRF1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications". Current Pharmaceutical Design. 5 (5): 289–315. doi:10.2174/138161280505230110095255. PMID 10213797.