Sweetman A J, Esmail A F
Methods Find Exp Clin Pharmacol. 1982;4(5):299-305.
In vitro studies of the effect of alphaxalone on ADP-stimulated respiration and Ca2+ uptake in rat brain mitochondria showed that the anesthetic was a potent inhibitor of both reactions. In vivo measurements showed that although alphaxalone did not inhibit oxidative phosphorylation during anaesthesia, the uptake of Ca2+ into the mitochondrial fraction was strongly inhibited. The degree of inhibition was dependent on the dose of anaesthetic administered and was reversed by the CNS stimulant, bemigride. Halothane and hexobarbitone also inhibited mitochondrial Ca2+ uptake in vivo. The levels of anaesthetic in the brain were determined after the administration of 14C-alphaxalone. There was no significant difference between the brain regions examined, but the levels reached were equal to those required to block CA2+ transport in isolated mitochondria.
关于α-羟孕酮对大鼠脑线粒体中ADP刺激的呼吸作用及Ca2+摄取影响的体外研究表明,该麻醉剂是这两种反应的强效抑制剂。体内测量结果显示,虽然α-羟孕酮在麻醉期间不抑制氧化磷酸化,但进入线粒体部分的Ca2+摄取受到强烈抑制。抑制程度取决于所给予麻醉剂的剂量,且可被中枢神经系统兴奋剂贝美格逆转。氟烷和己巴比妥在体内也抑制线粒体Ca2+摄取。给予14C-α-羟孕酮后测定了脑中的麻醉剂水平。所检查的脑区之间无显著差异,但所达到的水平与阻断分离线粒体中Ca2+转运所需的水平相当。