Key result
Cromakalim and pinacidil provoked concentration-dependent relaxations and increased 86Rb outflow in rat aortae, effects that were antagonized by hypoglycemic sulfonylureas like glibenclamide.
Hypoglycemic sulfonylureas antagonize the vasorelaxant effects of cromakalim and pinacidil in rat aortae, suggesting interference with vascular ATP-sensitive K+ channels.
Sulfonylureas may blunt KATP opener effects in diabetic patients; leaves open human vascular translation.
Cromakalim, pinacidil and nitroprusside provoked concentration-dependent relaxations of K(+)-depolarized rat aortae. Glibenclamide, tolbutamide and to a lesser extent tetraethylammonium antagonized the vasorelaxant action of cromakalim and pinacidil. Cromakalim, pinacidil but not nitroprusside elicited a marked increase in 86Rb outflow from preloaded and perifused aortic rings. These increases in 86Rb outflow were inhibited in a concentration-dependent manner by glibenclamide and tetraethylammonium. Our data extend previous observations indicating the involvement of K+ channels in the vasorelaxant properties of cromakalim and pinacidil. Moreover, the present findings suggest that both compounds could interfere with a vascular type of ATP-sensitive K+ channels.
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Lebrun et al. (2008) studied this question. Cromakalim and pinacidil vs. Nitroprusside and sulfonylureas was evaluated on Vasorelaxant action and 86Rb outflow. Cromakalim and pinacidil provoked concentration-dependent relaxations and increased 86Rb outflow in rat aortae, effects that were antagonized by hypoglycemic sulfonylureas like glibenclamide.
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