Fayle D R, Barritt G J, Bygrave F L
Biochem J. 1975 Jun;148(3):527-31. doi: 10.1042/bj1480527.
The effect of the local anaesthetic, butacaine, on adenine nucleotide binding and translocation in rat liver mitochondria partially depleted of their adenine nucleotide content was investigated. The range of butacaine concentrations that inhibit adenine nucleotide translocation and the extent of the inhibition are similar to the values obtained for native mitochondria. Butacaine does not alter either the total number of atractyloside-sensitive binding sites of depleted mitochondria, or the affinity of these sites for ADP or ATP under conditions where a partial inhibition of the rate of adenine nucleotide translocation is observed. The data are consistent with an effect of butacaine on the process by which adenine nucleotides are transported across the mitochondrial inner membrane rather than on the binding of adenine nucleotides to sites on the adenine nucleotide carrier. The results are briefly discussed in relation to the use of local anaesthetics in investigations of the mechanism of adenine nucleotide translocation.
研究了局部麻醉药布他卡因对腺嘌呤核苷酸含量部分耗尽的大鼠肝线粒体中腺嘌呤核苷酸结合和转运的影响。抑制腺嘌呤核苷酸转运的布他卡因浓度范围及其抑制程度与天然线粒体获得的值相似。在观察到腺嘌呤核苷酸转运速率部分受抑制的条件下,布他卡因既不改变耗尽线粒体中对苍术苷敏感的结合位点总数,也不改变这些位点对ADP或ATP的亲和力。数据表明布他卡因对腺嘌呤核苷酸跨线粒体内膜转运过程有影响,而不是对腺嘌呤核苷酸与腺嘌呤核苷酸载体上位点的结合有影响。结合局部麻醉药在腺嘌呤核苷酸转运机制研究中的应用对结果进行了简要讨论。