l型钙通道的特点拉西地封锁的豚鼠心室细胞。

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Cerbai E, Giotti Mugelli

l型钙通道的特点拉西地封锁的豚鼠心室细胞。

Br J杂志。1997年2月,120 (4):667 - 75。doi: 10.1038 / sj.bjp.0700951。

PubMed ID

9051306 (在PubMed

]

文摘

1。Ca(2 +)对抗拉西的属性进行膜片箝豚鼠心室细胞。2。在基础条件,0.1 microM拉西地减少了动作电位持续时间,与L型钙电流下降(ICa L) 66 + / - 4%的控制价值,没有电流电压的变化关系。背景电流和钠钾电流没有影响。所有的2分钟内达到一个稳定状态的影响。3。Ca(2 +)拉西是压敏电阻器:拮抗效应显著的消极转变(约20 mV)稳态失活曲线观察长(10)调节前脉冲,而不是较短(350毫秒)前脉冲。beplayapp4所示。压敏效应的出现和恢复造成0.1 microM拉西相比明显慢的equiactive nimodipine浓度(0.5 microM), nisoldipine (0.1 microM)。ICa L测量前脉冲后少-40 mV持续500毫秒或持平(95 + / - 5%的最大电流值)降低到49 + / - 10%时由nisoldipine nimodipine 43 + / - 9% (P < 0.05)和拉西地。 5. Similarly, the recovery from block in the presence of lacidipine was slower than with nimodipine and nisoldipine. After a prepulse of 1 s at -80 mV, ICa,L recovered up to 54 +/- 2% of the maximum current value in the presence of lacidipine, and up to 91 +/- 3% and 93 +/- 5% in the presence of nimodipine and nisoldipine, respectively (P < 0.05 vs lacidipine). 6. Blockade of ICa,L by lacidipine was use-dependent. After ten 200 ms long pulses (1 Hz) from -80 mV, ICa,L was reduced to 55 +/- 7% of the current measured at the first pulse. In the presence of nimodipine and nisoldipine, ICa,L elicited by the tenth pulse amounted to 93 +/- 3% and 80 +/- 6% of the first pulse value, respectively (P < 0.05 vs lacidipine). Lacidipine did not cause use-dependent blockade of ICa,L in cells stimulated with 10 ms long pulses. 7. These results demonstrate that lacidipine selectively inhibits ICa,L in isolated cardiomyocytes and suggest that this effect occurs mainly through binding to the inactivated Ca2+ channels.

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药物

拉西

药物靶点

药物	目标	类	生物	药理作用	行动
拉西	压敏电阻器l型钙通道(蛋白质组)	蛋白质组	人类	是的	拮抗剂	细节