The interaction between Mammalian Alkaloids and Anesthetics : Anesthetic Tolerance Associated with Alcohol Drinking and Prediction by Hair Analysis

哺乳动物生物碱与麻醉药之间的相互作用：与饮酒相关的麻醉耐受性和通过头发分析进行预测

基本信息

批准号：
15592145
负责人：
TSUCHIYA Hironori
金额：
$ 1.79万
依托单位：
Asahi University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2003
资助国家：
日本
起止时间：
2003 至 2005
项目状态：
已结题

项目摘要

Concerning anesthetic tolerance associated with drinking, the pharmacological background and prediction method were studied with focusing on the interaction with mammalian alkaloidal β-carbolines. A series of results were applied to various investigations on anesthetic effect change and biomembrane-drug interaction.1.Certain β-carbolines acted on membrane lipids to inhibit the membrane fluidization by local and general anesthetics. Such inhibition disappeared by their hepatic hydroxylation metabolism. It is speculated that anesthetic effects are decreased by the interaction with membrane-active β-carbolines increased in vivo by drinking.2.In the newly developed HPLC, the β-carboline concentrations in human scalp hair were found to significantly increase in chronic alcoholics. The potent interaction with β-carbolines to influence anesthesia may be predicted by hair analysis.3.Local anesthetics showed the reversed-phase chromatographic retention and membrane-fluidizing activity relations … More hips. Based on the hydrophobic interaction underlying membrane fluidization, the changes in anesthetic effects are simulated by HPLC analysis.4.The hydrophobic interaction of local anesthetics was applied to infusion balloons, which adsorbed local anesthetics immediately after injection to decrease their concentrations in effluents. Attention should be given to such adsorption so as not to influence clinical effects.5.The membrane-fluidizing effects of local anesthetics were induced under inflammatory acidic conditions and inhibited by inflammatory peroxynitrite, conflicting with the conventional hypothesis. The alternative mechanism should be theorized for the anesthetic failure in inflamed tissues.6.Nerve cell model membranes were fluidized by lidocaine ionic quaternary ammonium derivative and stereostructure-specifically fluidized by S(-)-,R(+)- and racemic bupivacaine and ropivacaine. The interaction with membrane lipids is responsible for the effects of local anesthetics in addition to that with ion channel/receptor proteins.7.Anesthetic-relating drugs, including new selective β-blockers and phenolic agents, showed the structure-selective membrane-activity, suggesting that the modification of membrane fluidity mechanistically contributes to their effects. Less

关于与饮酒相关的麻醉耐受性，研究了药物背景和预测方法，重点是与哺乳动物生物碱β-碳酸盐的相互作用。一系列结果应用于麻醉效应变化和生物膜 - 药物相互作用的各种投资。1。确定β-果蛋白作用于膜脂质上，以抑制局部和一般麻醉剂的膜流体。这种抑制作用因其肝羟基代谢消失。据推测，通过饮用与膜活性β果蛋白的相互作用减少了麻醉效应。头发分析可以预测与β-碳纤维蛋白影响麻醉的潜在相互作用。3。局部麻醉药表明，相反的相相色谱保留和膜 - 荧光荧光透明活性关系……更多的臀部。基于HPLC分析模拟麻醉作用的基础疏水相互作用。4。将局部麻醉药的疏水相互作用应用于输注球，后者在注射后立即吸附了局部麻醉药以降低其浓度以降低其浓度。应注意这种吸附，以免影响临床作用。5。局部麻醉剂的膜 - 荧光效应在炎症性酸性条件下诱导，并受到炎症性过氧硝酸盐的抑制，与常规假设相抵触。应从理论上将替代机制用于发炎组织中的麻醉衰竭。6。膜模型膜通过利多卡因离子季季铵衍生物流体化，由S（ - ） - ，R（+） - 和星期Bupivacaine和Ropivacaine和sacemocial Bupivacaine and Ropivacaine s（ - ） - ，R（ - ） - 与膜脂质的相互作用还负责局部麻醉剂的作用，除了与离子通道/受体蛋白相互作用。7.AnesthettheticResconticatients的药物，包括新的选择性β受体阻滞剂和酚类药物，还表明了结构性膜选择性的膜运动活性，表明其对膜流体的效果的修饰作用。较少的