Y-26763

Y-26763 is an activator of ATP-sensitive potassium (K_ATP) channels.¹ It increases the frequency of K_ATP channel openings in the presence of ATP and activates K_ATP channel currents in isolated human β-cells when used at a concentration of 200 μM. It also inhibits increases in intracellular calcium induced by histamine or norepinephrine (Item No. 16673) in isolated rabbit mesenteric artery smooth muscle in a concentration-dependent manner.² Y-26763 induces relaxation in isolated precontracted rat aortic rings (IC₅₀ = 0.027 μM).³ It decreases mean blood pressure in spontaneously hypertensive rats when administered intravenously at a dose of 0.03 mg/kg, an effect that can be reversed by glibenclamide (Item No. 15009).

WARNING This product is not for human or veterinary use.

1. Cosgrove, K.E., Straub, S.G., Barnes, P.D., et al. Y-26763: ATP-sensitive K⁺ channel activation and the inhibition of insulin release from human pancreatic beta-cells. Eur. J. Pharmacol. 486(2), 133-139 (2004).

2. Watanabe, Y., Suzuki, A., Suzuki, H., et al. Effect of membrane hyperpolarization induced by a K⁺ channel opener on histamine-induced Ca²⁺ mobilization in rabbit arterial smooth muscle. Br. J. Pharmacol. 117(6), 1302-1308 (1996).

3. Nakajima, T., Shinohara, T., Yaoka, O., et al. Y-27152, a long-acting K⁺ channel opener with less tachycardia: Antihypertensive effects in hypertensive rats and dogs in conscious state. J. Pharmacol. Exp. Ther. 261(2), 730-736 (1992).