Glyburide (Glibenclamide) - CAS 10238-21-8
Catalog number: 10238-21-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Potassium Channel
Glyburide (Glibenclamide) is an anti-diabetic compound in a class of medications known as sulfonylureas, closely related to sulfa agents.
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1. Effects of glyburide (glibenclamide) on myocardial function in Langendorff perfused rabbit heart and on myocardial contractility and slow calcium current in guinea-pig single myocytes
Said Y. Khatib and Mark R. Boyett. Molecular and Cellular Biochemistry 242: 81–87, 2003.
The anti-diabetic sulfonylurea drugs, like glyburide, have been established as potent blockers of ATP dependent potassium channel (K+ATP) in the heart. They have been reported to cause positive inotropic effect in animals and human. Linden and Brooker reported a significant and large increase in contractility after an initial decrease in rabbit atrial muscle. Tolbutamide, first generation of sulfonylurea agent, was shown to have positive inotropic effect and to dramatically improve the recoverability of myocardial function of ischemic myocardium, which was suggested to be a cause of increased cardiac mortality. Glyburide, a second generation of sulfonylurea agent, was shown to have a positive inotropic effect in healthy volunteers. It produced a significant increase in myocardial contractility as indicated by increased ejection fraction and increased cardiac work. We reported a significant positive inotropic action for glyburide as shown by increased left ventricular pressure produced by 10 µM, in Langendorff isolated rabbit heart under normoxic conditions of perfusion. Glibenclamide elicited sustained positive inotropic effect in isolated guinea pig heart, improved functional recovery of ischemic myocardium at 45 min reperfusion and accelerated the onset of contracture thus speeding up cardiac arrest in rat and guinea-pig heart. Recently, glibenclamide was shown to increase intracellular calcium concentration in a dose dependent manner in cardiomyocytes. Smallwood et al. reported that glibenclamide attenuated action potential shortening (APD) during ischemia in a dose-related manner, but it did not effect on APD of the rabbit left ventricle. However, glyburide increased action potential duration at 95% repolarization in normoxic canine purkinje fibers.
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CAS 10238-21-8 Glyburide (Glibenclamide)

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