The inhibitory effects of calmodulin antagonists on the endothelium-dependent relaxation in rabbit aorta.

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Nagase, H., Karaki, H. and Urakawa, N. The inhibitory effects of calmodulin antagonists on the endothelium-dependent relaxation in rabbit aorta . Japanese Journal of Smooth Muscle Research 1986, 22 (2), 97-102 .-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 (10-6-10-5 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 endoth -elium-derived relaxing factor involves the process mediated by calmodulin in the rabbit aorta.
日本平滑筋学会の論文