65321-41-7

MK761 is a new class of compound which has beta adrenoceptor antagonist and vasodilating properties in a single molecule. The compound has in vitro beta adrenoceptor blocking activity in the isolated cat heart papillary muscle and isolated rat atria. It is approximately as potent as timolol and pindolol in blocking cardiac and vascular beta adrenergic receptors.

MK-761 free base is a potent and orally active β2-adrenergic blocker. MK-761 free base shows antihypertensive and positive inotropic effects. MK-761 free base shows vasodilating properties[1].

Beta-2 adrenergic receptor

[1] Scriabine A, et al. Antihypertensive and cardiac effects of two novel beta-adrenoceptor blocking drugs. Experientia. 1979 Dec 15;35(12):1634-7. DOI:10.1007/BF01953238
[2] C.S. Sweet, et al. Peripheral Vasodilator and β-Adrenoceptor Blocking Properties of Several β-Adrenoceptor Antagonists. Clinical and Experimental Hypertension. 2009, 449-471.
[3] Sweet CS, et al. Beta adrenoceptor blocking properties of MK-761. J Pharmacol Exp Ther. 1979 Oct;211(1):195-9. PMID:40012