Description
Efaroxan hydrochloride is an antagonist at α2-adrenergic receptors and imidazoline-1 receptors. Efaroxan hydrochloride administration in animal models of opioid use shows a potential role for α2-adrenergic receptors in opioid-mediated mechanisms of tolerance and antinociception. This compound also exhibits antihyperglycemic activity, improving oral glucose tolerance in animal models of diabetes due to its ability to inhibit K(ATP) K+ channels on pancreatic beta cells. Additionally, administration of efaroxan hydrochloride shows benefit in animal models of Parkinson’s Disease.
References
Milne B, Jhamandas K, Sutak M, et al. Stereo-selective inhibition of spinal morphine tolerance and hyperalgesia by an ultra-low dose of the alpha-2-adrenoceptor antagonist efaroxan. Eur J Pharmacol. 2013 Feb 28;702(1-3):227-34. PMID: 23376415.
Lehner Z, Stadlbauer K, Adorjan I, et al. Mechanisms of antihyperglycaemic action of efaroxan in mice: time for reappraisal of α2A-adrenergic antagonism in the treatment of type 2 diabetes? Diabetologia. 2012 Nov;55(11):3071-82. PMID: 22898767.
Le Brigand L, Virsolvy A, Manechez D, et al. In vitro mechanism of action on insulin release of S-22068, a new putative antidiabetic compound. Br J Pharmacol. 1999 Nov;128(5):1021-6. PMID: 10556939.
Chopin P, Colpaert FC, Marien M. Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J. Pharmacol. Exp. Ther. 1999. 288 (2): 798–804. PMID 9918591.
Chan SL, Dunne MJ, Stillings MR, et al. The alpha 2-adrenoceptor antagonist efaroxan modulates K+ATP channels in insulin-secreting cells. Eur J Pharmacol. 1991 Oct 29;204(1):41-8. PMID: 1687123.