Kurasu 3 Kofuseimyakuyaku MS-551 No Ieusagi Shinshitsukin Ni Taisuru Denki Seirigakuteki Sayo (Electrophysiological Effects of MS-551, a New Class 3 Antiarrhythmic Agent, on Isolated Rabbit Ventricular Muscles)
(Englisch)
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MS-511, 1, 3-dimethyl 6-(2-(N-(2-hydroxethyl) 3-(4-nitrophenyl) propylamino) ethylamino) 2, 4-(1H, 3H)-pyrimidinedione hydrochloride, is a newly developed antiarrhythmic agent that can prolong the Action Potential Duration (APD) and effective refractory period mainly due to K channel blockage. The MS-551 was compared with sotalol and E-4031 in respect to prolongation of effective refractory period. Rabbit ventricular muscles were extracted, perfusated with perfusate containing MS-551, and the membrane potential was measured. As a result, MS-551 prolonged APD significantly at the concentration of 0.3 micro-M or more, without suppressing maximum upstroke velocity. The APD prolongation caused by sotalol and E-4031 showed remarkable reverse use-dependency within the range of 0.1 to 3.0 Hz of stimulus, whereas that by MS-551 showed diphasic rate-dependency. This suggests that MS-511 may suppress a different K channel from other drug suppression. Among various K channels in the myocytes, slow rectifying K channel may participate in the rate-dependent APD prolongation, and MS-551 may bind with the activated K channel because the effect emerged not at the first stimulating pulse but at the second pulse after a long pause.
Kurasu 3 Kofuseimyakuyaku MS-551 No Ieusagi Shinshitsukin Ni Taisuru Denki Seirigakuteki Sayo (Electrophysiological Effects of MS-551, a New Class 3 Antiarrhythmic Agent, on Isolated Rabbit Ventricular Muscles)