新钾通道开放剂BPDZ 79对离体主动脉的扩血管作用

Vasodilative properties of BPDZ 79, a new potassium channel opener, in isolated aorta.

AIM: To compare the effect of a novel potassium channel opener 3-(1',2',2'-trimethylpropyl)amine-4H-pyrido (2,3-e)-1,2,4-thiadiazine, 1-dioxide (BPDZ 79), with diazoxide on aorta. METHODS: Muscle tension of rat aorta was compared with adjacent aortic rings without endothelium. One ring was precontracted with KCl 80 mmol.L-1. Three rings were precontracted with KCl 80 mmol.L-1, and two of them were incubated with glibenclamide (0, 1, and 10 mumol.L-1). 86Rb outflow from rat aorta was measured in the presence of glibenclamide 10 mumol.L-1. RESULTS: BPDZ 79 and diazoxide provoked concentration-dependent and endothelium-independent relaxation of the vasoconstriction evoked by KCl 30 mmol.L-1, but not by 80 mmol.L-1. BPDZ 79 showed more potent vasorelaxation and 86Rb outflow than diazoxide. After incubation with glibenclamide (1 and 10 mumol.L-1), an inhibitor of the ATP-sensitive K+ channels, the relaxation induced by BPDZ 79 and diazoxide were decreased with the same pattern. CONCLUSION: BPDZ 79 is a potent vasodilator by opening potassium channels.