Ca2+通道激活剂CGP28392对大鼠心肌的双相变力作用：与细胞内Ca2+释放的可能关系。
Biphasic inotropic effects of a Ca2+ channel activator CGP28392 in rat myocardium: possible relation to intracellular Ca2+ release.
作者信息
Kobrinsky E, Saxon M
机构信息
Institute of Biological Physics, Acad. Sci. of the USSR, Pushchino.
出版信息
Br J Pharmacol. 1987 Nov;92(3):499-504. doi: 10.1111/j.1476-5381.1987.tb11349.x.
Abstract
- The inotropic effect of a Ca2+-entry stimulator, CGP28392, (CGP) was compared in rat and frog myocardium in a concentration- and time-dependent manner. 2. Frog preparations exhibited a persistent positive inotropic effect following prolonged treatment with CGP. 3. Compared to amphibian myocardium, rat ventricular muscle exhibited a biphasic time-dependent response to CGP: an initial increase in the twitch tension amplitude of 30% was changed to a reduction of 80% below the control level during prolonged exposure to CGP (stimulation frequency, 0.2 Hz). 4. Following prolonged incubation with CGP, the resting-state contraction was decreased and the negative force-frequency relation was converted into a positive one in rat muscle. 5. Since sarcoplasmic reticulum (SR) is the major source of Ca2+ in a rested-state contraction, inhibition by CGP suggests an additional, intracellular action of the Ca2+ channel activator on SR-Ca2+ release in rat myocardium.
摘要
- 以浓度和时间依赖性方式比较了钙内流刺激剂CGP28392（CGP）对大鼠和青蛙心肌的变力作用。2. 在用CGP进行长时间处理后，青蛙标本表现出持续的正性变力作用。3. 与两栖类心肌相比，大鼠心室肌对CGP表现出双相时间依赖性反应：在长时间暴露于CGP（刺激频率为0.2 Hz）期间，抽搐张力幅度最初增加30%，随后降至对照水平以下80%。4. 在用CGP进行长时间孵育后，大鼠肌肉的静息状态收缩减弱，负性力-频率关系转变为正性关系。5. 由于肌浆网（SR）是静息状态收缩时Ca2+的主要来源，CGP的抑制作用表明钙通道激活剂对大鼠心肌中SR-Ca2+释放有额外的细胞内作用。
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