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Potential-dependent inhibition of cardiac Ca2+ inward currents by Ro 40-5967 and verapamil: relation to negative inotropy.

作者信息

Fang L M, Osterrieder W

机构信息

Pharmaceutical Research Department, F. Hoffmann-La Roche Ltd., Basel, Switzerland.

出版信息

Eur J Pharmacol. 1991 Apr 17;196(2):205-7. doi: 10.1016/0014-2999(91)90430-x.

DOI:10.1016/0014-2999(91)90430-x
PMID:1651875
Abstract

Ro 40-5967 is a structurally novel Ca2+ channel blocker which binds to the [3H]desmethoxyverapamil receptor in cardiac membranes with a potency similar to that of verapamil but which has considerably fewer negative inotropic effects. In the present study, the inward Ca2+ current was measured in isolated myocytes with the whole-cell patch-clamp technique. It was found that at a physiological membrane potential (-80 mV) Ro 40-5967 was also less potent than verapamil in inhibiting this current, and that negative inotropy and Ca2+ channel blockade were correlated.

摘要

相似文献

1
Potential-dependent inhibition of cardiac Ca2+ inward currents by Ro 40-5967 and verapamil: relation to negative inotropy.
Eur J Pharmacol. 1991 Apr 17;196(2):205-7. doi: 10.1016/0014-2999(91)90430-x.
2
The structurally novel Ca2+ channel blocker Ro 40-5967, which binds to the [3H] desmethoxyverapamil receptor, is devoid of the negative inotropic effects of verapamil in normal and failing rat hearts.结构新颖的钙离子通道阻滞剂Ro 40 - 5967可与[3H]去甲氧基维拉帕米受体结合，在正常和衰竭的大鼠心脏中，它没有维拉帕米的负性肌力作用。
Cardiovasc Drugs Ther. 1990 Jun;4(3):731-6. doi: 10.1007/BF01856562.
3
In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action.新型钙通道阻滞剂Ro 40-5967的体外药理学特性：具有强效血管舒张作用但正性肌力作用较弱
J Cardiovasc Pharmacol. 1989 May;13(5):754-9.
4
T- and L-type Ca2+-channel antagonists reduce contractility in guinea pig cardiac myocytes.T型和L型钙离子通道拮抗剂可降低豚鼠心肌细胞的收缩性。
J Cardiovasc Pharmacol. 1998 Aug;32(2):323-30. doi: 10.1097/00005344-199808000-00022.
5
Mibefradil (Ro 40-5967) blocks multiple types of voltage-gated calcium channels in cultured rat spinal motoneurones.米贝地尔（Ro 40-5967）可阻断培养的大鼠脊髓运动神经元中多种类型的电压门控钙通道。
Cell Calcium. 1997 Oct;22(4):299-311. doi: 10.1016/s0143-4160(97)90068-3.
6
Effects of mibefradil, a blocker of T-type Ca2+ channels, in single myocytes and intact muscle of guinea-pig heart.T型钙通道阻滞剂米贝拉地尔对豚鼠心脏单个心肌细胞和完整心肌的作用。
J Physiol Pharmacol. 1998 Dec;49(4):577-90.
7
Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967).通过钙通道拮抗剂米贝地尔（Ro 40 - 5967）对非洲爪蟾卵母细胞中表达的多种类型电压门控钙通道进行电压依赖性阻断。
Mol Pharmacol. 1995 Sep;48(3):540-9.
8
Ca2+ channel actions of the non-dihydropyridine Ca2+ channel antagonist Ro 40-5967 in vascular muscle cells cultured from dog coronary and saphenous arteries.非二氢吡啶类钙离子通道拮抗剂Ro 40-5967在犬冠状动脉和隐静脉培养的血管平滑肌细胞中的钙离子通道作用
Naunyn Schmiedebergs Arch Pharmacol. 1993 Aug;348(2):191-6. doi: 10.1007/BF00164798.
9
Effects of the novel T-type calcium channel antagonist mibefradil on human myocardial contractility in comparison with nifedipine and verapamil.新型T型钙通道拮抗剂米贝拉地尔与硝苯地平及维拉帕米相比对人心肌收缩力的影响
J Cardiovasc Pharmacol. 1997 May;29(5):692-6. doi: 10.1097/00005344-199705000-00019.
10
Interaction of Ro 40-5967 and verapamil with the stably expressed alpha 1-subunit of the cardiac L-type calcium channel.
J Pharmacol Exp Ther. 1995 Jul;274(1):54-63.

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Management of calcium channel antagonist overdose.
钙通道拮抗剂过量的处理
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5
Effects of mibefradil on intracellular Ca2+ release in cultured rat cardiac fibroblasts and human platelets.米贝拉地尔对培养的大鼠心脏成纤维细胞和人血小板细胞内钙离子释放的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):94-101. doi: 10.1007/BF00168921.
6
Expression of the L-type calcium channel with two different beta subunits and its modulation by Ro 40-5967.具有两种不同β亚基的L型钙通道的表达及其受Ro 40-5967的调节。
Pflugers Arch. 1995 Jan;429(3):400-11. doi: 10.1007/BF00374156.
7
The interaction of the calcium antagonist RO 40-5967 with digoxin.钙拮抗剂RO 40-5967与地高辛的相互作用。
Br J Clin Pharmacol. 1995 May;39(5):491-6. doi: 10.1111/j.1365-2125.1995.tb04485.x.