Tong Q S, Xia G J, Yao W X, Jiang M X, Bai X C, Bao Y D
Department of Pharmacology, School of Basic Medical Science, Tongji Medical University, Wuhan.
Yao Xue Xue Bao. 1996;31(11):867-71.
The effects of benzyltetrahydropalmatine (BTHP) on delayed rectified K+ currents (Ik) expressed in Xenopus oocytes and Ik of toad (Bufo bufo gargarizans) oocytes were studied. The Ik expressed in Xenopus oocytes was measured after microinjection of mRNA isolated from carp fish (C anratus L.) brains with double -microelectrode voltage clamp technique. The maximum and mean value of Ik expressed in Xenopus oocytes were 600 nA and 360 +/- 104 nA, respectively. BTHP reduced the current amplitude of Ik expressed in Xenopus oocytes in 10-1000 mumol.L-1 dose-dependently, EC50 was 29 mumol.L-1. Also, the reduction of Ik of toad oocytes was 9.1%, 29.1%, 54.7% and 68.6% by BTHP 10, 30, 100 and 1000 mumol.L-1, respectively, EC50 was 33 mumol.L-1. The results showed that BTHP possesses an inhibitory effect on Ik, the main ion mechanism of antiarrhythmic action of BTHP.
研究了苄基四氢巴马汀(BTHP)对非洲爪蟾卵母细胞表达的延迟整流钾电流(Ik)以及中华大蟾蜍卵母细胞Ik的影响。采用双微电极电压钳技术,在显微注射从鲤鱼脑分离的mRNA后,测量非洲爪蟾卵母细胞中表达的Ik。非洲爪蟾卵母细胞中表达的Ik的最大值和平均值分别为600 nA和360±104 nA。BTHP在10 - 1000 μmol·L-1剂量依赖性地降低非洲爪蟾卵母细胞中表达的Ik电流幅度,半数有效浓度(EC50)为29 μmol·L-1。此外,10、30、100和1000 μmol·L-1的BTHP分别使中华大蟾蜍卵母细胞的Ik降低9.1%、29.1%、54.7%和68.6%,EC50为33 μmol·L-1。结果表明,BTHP对Ik具有抑制作用,这是BTHP抗心律失常作用的主要离子机制。