Antalarmin (hydrochloride)

Corticotropin-releasing hormone (CRH) secreted from the hypothalamus is the major regulator of pituitary corticotropin-release and consequent glucocorticoid secretion. Antalarmin is a selective, nonpeptide antagonist of the CRH receptor 1 (K_i = 1 nM) that, consequently, reduces the release of corticotropin in response to chronic stress.¹ Through its antagonism of central CRH signaling, antalarmin can reduce endocrinological, cardiovascular, and behavioral responses to stressful stimuli.² It has also been shown to reduce dose escalation in cocaine-addicted rats, to produce anti-inflammatory effects in arthritis models, and to suppress stress-induced gastric ulceration related to irritable bowel syndrome.^2,3

WARNING This product is not for human or veterinary use.

1. Webster, E.L., Lewis, D.B., Torpy, D.J., et al. 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), 5747-5750 (1996).

2. Deak, T., Nguyen, K.T., Ehrlich, A.L., et al. The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress. Endocrinology 140(1), 79-86 (1999).

3. Fahmy, H., Spyridaki, K., Kuppast, B., et al. The "homeostasis hormone" and its CRF1 receptor. From structure to function. Hormones (Athens) 11(3), 254-271 (2012).