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目的·研究(S)-OTS·HCl对心脏生物电活动的影响。方法·运用细胞内生物电记录、心电图及Langendorff心脏灌流技术,在离体和在体情况下研究(S)-OTS·HCl对豚鼠和家兔心脏的作用。结果·(S)-OTS·HCl可与M_2型胆碱能受体结合,并在动物整体心电图记录中剂量依赖性地延长RR间期。(S)-OTS·HCl对心室肌的静息电位(RP)、动作电位幅值(APA)和动作电位最大上升速率(V_(max))没有影响,但(S)-OTS·HCl(1×10~(-5) mol/L)可显著缩短动作电位时程APD_(50)和APD_(90)分别至91.6%和90.9%。当(S)-OTS·HCl(1×10~(-7) mol/L)灌流家兔窦房结标本时,可使4期自动除极速率缩短至13.7%,也可有效抑制钙通道,并使窦房结自律性动作电位的APA和V_(max)减小。离体心肌收缩力亦随(S)-OTS·HCl的剂量增加而降低。结论·(S)-OTS·HCl是一个作用较强的胆碱能受体激动剂,能与心肌M_2受体结合,产生负性变时、变力和变传导效应。
Objective · To investigate the effect of (S) -OTS · HCl on cardiac bioelectric activity. METHODS • The effects of (S) -OTS · HCl on guinea pig and rabbit hearts were studied ex vivo and in vivo using intracellular bioelectrical recordings, electrocardiograms, and Langendorff cardioplegia. Results (S) -OTS · HCl binds to the cholinergic receptors type M_2 and prolongs the RR interval dose-dependently in animal whole-body electrocardiographic recordings. (S) -OTS · HCl had no effect on ventricular resting potential (RP), action potential amplitude (APA) and maximum rate of action potential (V max) × 10 ~ (-5) mol / L) could shorten the action potential duration APD_ (50) and APD_ (90) to 91.6% and 90.9%, respectively. When (S) -OTS · HCl (1 × 10 ~ (-7) mol / L) perfusion of rabbit sinoatrial node specimens, can make the four automatic depolarization rate reduced to 13.7%, but also can effectively inhibit the calcium channel, And reduce the APA and Vmax of the self-regulated action potentials of the sino-atrial node. The contractile force of isolated myocardium also decreased with the dose of (S) -OTS · HCl. CONCLUSION · (S) -OTS · HCl is a powerful cholinergic receptor agonist that binds to M 2 receptors in the myocardium to produce negative variable, variable and variable conductance effects.