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溴哌维林、氯化锰和D600对大鼠子宫平滑肌电活动和机械活动影响的比较。

Comparison of pinaverium bromide, manganese chloride and D600 effects on electrical and mechanical activities in rat uterine smooth muscle.

作者信息

Mironneau J, Lalanne C, Mironneau C, Savineau J P, Lavie J L

出版信息

Eur J Pharmacol. 1984 Feb 10;98(1):99-107. doi: 10.1016/0014-2999(84)90113-4.

Abstract

The effects of pinaverium bromide, were compared with those of D600 and manganese chloride (Mn), on membrane potentials, ionic currents and isometric contractions in uterine smooth muscle strips from pregnant rats. Pinaverium bromide (10(-7) - 10(-6) M) depressed twitch contractions and K-contractures within 15-20 min while D600 (2 X 10(-6) M) and Mn (10(-3) M) abolished both contractions. D600 and pinaverium bromide were more potent inhibitors in K-depolarized preparations than in polarized tissues. At a supramaximal dose (10(-5) M), pinaverium bromide decreased the rate of rise, amplitude, and rate of repolarization of the action potential, and prolonged the potential duration. The inward Ca current was depressed and the reduction in Cai was responsible for the decrease in K current. Pinaverium bromide (10(-5) M) depressed the myometrial contractions induced in Ca-free solution by acetylcholine (10(-4) M) and by prolonged membrane depolarizations. Mn (2.5 X 10(-3) M) only reduced the Ach-induced contraction and D600 (10(-5) M) had no effect on intracellular Ca stores. The results indicate that pinaverium bromide has Ca channel blocking properties similar to those of currently used Ca antagonists; it may also exert an effect to depress contractions supported by intracellular Ca release.

摘要

将溴哌维林的作用与D600和氯化锰(Mn)对妊娠大鼠子宫平滑肌条的膜电位、离子电流和等长收缩的作用进行了比较。溴哌维林(10^(-7)-10^(-6)M)在15-20分钟内抑制了抽搐收缩和钾收缩,而D600(2×10^(-6)M)和Mn(10^(-3)M)则消除了这两种收缩。D600和溴哌维林在钾去极化制剂中比在极化组织中是更有效的抑制剂。在超最大剂量(10^(-5)M)时,溴哌维林降低了动作电位的上升速率、幅度和复极化速率,并延长了电位持续时间。内向钙电流被抑制,细胞内钙的减少是钾电流减少的原因。溴哌维林(10^(-5)M)抑制了无钙溶液中由乙酰胆碱(10^(-4)M)和长时间膜去极化诱导的子宫肌层收缩。Mn(2.5×10^(-3)M)仅降低了乙酰胆碱诱导的收缩,而D600(10^(-5)M)对细胞内钙储存无影响。结果表明,溴哌维林具有与目前使用的钙拮抗剂类似的钙通道阻断特性;它也可能发挥作用,抑制由细胞内钙释放支持的收缩。

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