抑制葡萄糖运输和直接与1型的互动使便利的葡萄糖转运体(GLUT-1)依托咪酯,氯胺酮、异丙酚:与巴比妥类药物进行比较。

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斯蒂芬森KN, Croxen RL, El-Barbary Fenstermacher JD, Haspel HC

抑制葡萄糖运输和直接与1型的互动使便利的葡萄糖转运体(GLUT-1)依托咪酯,氯胺酮、异丙酚:与巴比妥类药物进行比较。

生物化学杂志。2000年9月1;60 (5):651 - 9。

PubMed ID

10927023 (在PubMed

]

文摘

氯胺酮、依托咪酯、异丙酚和戊巴比妥比较1型的影响和交互使便利的葡萄糖转运体(GLUT-1)。通量的放射性标记的己糖被用来确定麻醉剂对GLUT-1功能的影响。低渗的人类红细胞的溶血是用来评估扰动膜的完整性。淬火的内在蛋白荧光被用来评估与纯化GLUT-1麻醉剂的直接交互。戊巴比妥,氯胺酮、依托咪酯、异丙酚抑制小鼠成纤维细胞的葡萄糖运输IC(50)值为0.8,1。6、0.1和0.4毫米。戊巴比妥、氯胺酮、依托咪酯、异丙酚也抑制人类红细胞糖运输。戊巴比妥的IC(50)值和氯胺酮底物的平衡依赖展出交换而不是单向流出。这不是观察依托咪酯。异丙酚并没有抑制平衡交换但抑制单向流出衬底的依赖。 Pentobarbital protected against hemolysis, whereas etomidate and ketamine promoted hemolysis of erythrocytes. Propofol had no effect on membrane integrity. Pentobarbital, ketamine, and etomidate all interacted directly with GLUT-1, with apparent K(d) values of 2.2, 0.8, and 0.5 mM, respectively. Like barbiturates, ketamine, etomidate, and propofol inhibited GLUT-1 at concentrations near to those used pharmacologically. Inhibition of GLUT-1 by these intravenous general anesthetics was complex, exhibiting differential kinetic effects on equilibrium exchange versus unidirectional fluxes and contrasting substrate dependencies. Like barbiturates, ketamine and etomidate bound to GLUT-1 with affinities that paralleled inhibition of glucose transport. As a class, intravenous general anesthetics, in contrast to inhalation anesthetics, inhibit GLUT-1-mediated glucose transport.

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药物载体

药物	航空公司	类	生物	药理作用	行动
依托咪酯	溶质载体家庭2,促进葡萄糖转运体1成员	蛋白质	人类	未知的	抑制剂	细节