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向细胞内注入微量钙,可使肌肉出现收缩反应,证实了在平滑肌的兴奋—收缩偶联过程中,钙具有非常重要的作用。Fleckenstein于60年代首先发现异搏定(Verapamil)和心可定(Prenylamine)对电刺激引起的肌肉收缩有明显的抑制作用,但直到1969年建立了可分别测定膜内、外Na~+和Ca~(++)流的方法以后,才确定这是一类独特的药物,可选择性的阻断细胞膜的慢钙流,并定名为钙通道阻断剂(又名钙拮抗剂)。这一发现引起了国际范围的注意,从而合成了一些新的、不同化学类型的钙拮抗剂。经过大量实验室和临床研究,
Injection of trace amounts of calcium into the cells can cause muscle contraction, confirming that calcium plays an important role in the excitation-contraction coupling of smooth muscle. Fleckenstein first discovered in the 1960s that Verapamil and Prenylamine significantly inhibited muscle contractions caused by electrical stimulation. However, until 1969, a series of assays were established to determine intra- and extracellular Na ~ + and Ca ~ (++) flow method, it was determined that this is a unique class of drugs that selectively block the slow calcium flow in the cell membrane and name it as a calcium channel blocker (aka calcium antagonist). This discovery has attracted international attention, resulting in the synthesis of some new, different types of chemical calcium antagonists. After a large number of laboratory and clinical research,