溴化匹那维铵对钙调蛋白调节功能的作用。

Action of pinaverium bromide on calmodulin-regulated functions.

作者信息

Wuytack F, De Schutter G, Casteels R

出版信息

Eur J Pharmacol. 1985 Aug 7;114(1):85-8. doi: 10.1016/0014-2999(85)90525-4.

Abstract

Pinaverium bromide at concentrations below 10(-5) M did not inhibit calmodulin-dependent enzymes such as phosphodiesterase and the Ca transport ATPase of the plasma membrane. At higher concentrations the compound interacted with the stimulation of those enzymes by calmodulin and also inhibited the calmodulin-independent activity. A similar inhibitory action was observed for the NaK ATPase. It is concluded that the inhibitory action of pinaverium bromide on smooth muscle concentration at concentrations below 10(-5) M was due to its interaction with the voltage-dependent Ca channels and not to its interference with the calmodulin-dependent activation of the contractile proteins.

摘要

浓度低于10⁻⁵ M的溴化匹那韦林不会抑制钙调蛋白依赖性酶，如磷酸二酯酶和质膜的钙转运ATP酶。在较高浓度下，该化合物与钙调蛋白对这些酶的刺激相互作用，并且还抑制了不依赖钙调蛋白的活性。对钠钾ATP酶也观察到类似的抑制作用。得出的结论是，浓度低于10⁻⁵ M时溴化匹那韦林对平滑肌收缩的抑制作用是由于其与电压依赖性钙通道的相互作用，而不是由于其干扰收缩蛋白的钙调蛋白依赖性激活。