Nagase H, Karaki H, Urakawa N
Nihon Heikatsukin Gakkai Zasshi. 1986 Apr;22(2):97-102. doi: 10.1540/jsmr1965.22.97.
Effects of trifluoperazine (TFP, 10(-5) M), trifluoperazine sulfoxide (TFP-SO, 10(-5) M), N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7-, 10(-4) M), N-(6-aminohexyl)-1-naphthalenesulfonamide (W-5, 10(-4) M) and verapamil (10(-5) M) on the endothelium-dependent relaxation of the contractions induced in the isolated rabbit aorta were studied. Carbachol (10(-6) - 10(-6) M) and A23187 (10(-8) M) relaxed the contraction due to norepinephrine (10(-6) M and histamine (10(-5) M) in the aorta with endothelium. TFP and W-7 completely inhibited the relaxation induced by carbachol and A23187. In contrast, TFP-SO and W-5, which have lower affinity to calmodulin, had little or no effect on either the carbachol- or A23187-induced relaxation. An organic calcium antagonist, verapamil, did not change the relaxation induced by carbachol or A23187. W-7 did not modify the relaxing effect of sodium nitroprusside (10(-8) - 10(-6) M) which is not mediated by endothelium. These results suggest that either formation or release of endothelium-derived relaxing factor involves the process mediated by calmodulin in the rabbit aorta.
研究了三氟拉嗪（TFP，10⁻⁵ M）、三氟拉嗪亚砜（TFP-SO，10⁻⁵ M）、N-(6-氨基己基)-5-氯-1-萘磺酰胺（W-7，10⁻⁴ M）、N-(6-氨基己基)-1-萘磺酰胺（W-5，10⁻⁴ M）和维拉帕米（10⁻⁵ M）对离体兔主动脉中诱导收缩的内皮依赖性舒张的影响。在有内皮的主动脉中，卡巴胆碱（10⁻⁶ - 10⁻⁶ M）和A23187（10⁻⁸ M）可舒张由去甲肾上腺素（10⁻⁶ M）和组胺（10⁻⁵ M）引起的收缩。TFP和W-7完全抑制了卡巴胆碱和A23187诱导的舒张。相比之下，对钙调蛋白亲和力较低的TFP-SO和W-5对卡巴胆碱或A23187诱导的舒张几乎没有影响。有机钙拮抗剂维拉帕米并未改变卡巴胆碱或A23187诱导的舒张。W-7并未改变由内皮非介导的硝普钠（10⁻⁸ - 10⁻⁶ M）的舒张作用。这些结果表明，内皮源性舒张因子的形成或释放涉及兔主动脉中由钙调蛋白介导的过程。
