Santillán A, Almanza J, Valenzuela F
Departamento de Fisiología del Instituto Nacional de Cardiología Ignacio Chávez, México, D.F.
Arch Inst Cardiol Mex. 1990 Jul-Aug;60(4):361-8.
Cyproheptadine is an antagonist of S1 serotoninergic and H1 histaminergic receptors, with a well known cardiovascular activity, mainly vasodilation and a negative chronotropic effect. It has been suggested that cyproheptadine as other antiserotoninergic drugs act by blocking the calcium channel. In order to explore this possibility the actions of this drug were studied in several cardiac preparations: sinus node, isolated ventricular myocytes and papillary muscle from guinea-pig's heart. The experiments were performed using the conventional recording techniques of intracellular electrical activity and isometric tension. Doses from 0.25 microM to 1.0 microM were studied. The main findings were: in sinus node: a) inhibition of automatic activity, b) a decrease in the upstroke, c) a decrease in the plateau level, and d) a shortening of the action potential. In isolated ventricular myocytes: a) a decrease in the rate of depolarization, b) a decrease in the plateau level and c) a shortening of the action potential. In the papillary muscle: a) a decrease in tension and b) a shortening of the action potential. All the effects observed were dose dependent an agree with a blockade of the calcium channel.
赛庚啶是5-羟色胺能和H1组胺能受体的拮抗剂,具有众所周知的心血管活性,主要是血管舒张和负性变时作用。有人提出,赛庚啶与其他抗5-羟色胺能药物一样,通过阻断钙通道发挥作用。为了探究这种可能性,在几种心脏标本中研究了该药物的作用:豚鼠心脏的窦房结、离体心室肌细胞和乳头肌。实验采用细胞内电活动和等长张力的传统记录技术进行。研究了0.25微摩尔至1.0微摩尔的剂量。主要发现如下:在窦房结中:a)自动活动受到抑制,b)上升支降低,c)平台期水平降低,d)动作电位缩短。在离体心室肌细胞中:a)去极化速率降低,b)平台期水平降低,c)动作电位缩短。在乳头肌中:a)张力降低,b)动作电位缩短。观察到的所有效应均呈剂量依赖性,且与钙通道阻断一致。