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目的:测定CPU-86017抑制哇巴因诱导的豚鼠心律失常和心率减慢的有效血浆浓度.方法:CPU-86017 ⅳ抑制哇巴因诱发心律失常.心率由ECG监护.用HPLC法测CPU-86017有效血浆浓度,用放免法测血浆中TXB_2及6-酮-PGF_(1α).结果:CPU-86017抑制哇巴因诱导的心律失常及减慢心率的血药浓度分别为0.13-0.23 mg/L及0.13-0.31 mg/L.CPU-86017 ⅳ降低血浆中TXB_2和升高血浆中6-酮-PGF_(1α).结论:CPU-86017的抑制心律失常和降低心率作用与血浆浓度呈相关性.
OBJECTIVE: To determine the effective plasma concentration of igabain-induced guinea-pig arrhythmia and heart rate reduction by CPU-86017.Methods: CPU-86017 ⅳ inhibits ouabain-induced arrhythmia and the heart rate is monitored by ECG.Using HPLC to measure CPU-86017 The plasma concentrations of TXB_2 and 6-keto-PGF_ (1α) in plasma were determined by radioimmunoassay.Results: The plasma concentrations of ouabain-induced arrhythmia and heart rate reductions were 0.13-0.23 mg / L And 0.13-0.31 mg / L.CPU-86017 ⅳ decreased TXB_2 in plasma and increased 6-keto-PGF_ (1α) in plasma.CONCLUSIONS: The effects of CPU-86017 on inhibiting arrhythmia and decreasing heart rate are correlated with plasma concentrations.