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[Review] Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol: Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects

https://asahi-u.repo.nii.ac.jp/records/1506
https://asahi-u.repo.nii.ac.jp/records/1506
f3296f68-51fd-473f-b44d-2338bdfb8afd
Item type 朝日大学 教育・研究業績(1)
公開日 2015-02-10
タイトル
タイトル [Review] Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol: Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects
言語
言語 eng
資源タイプ
資源タイプ識別子 http://purl.org/coar/resource_type/c_1843
資源タイプ other
アクセス権
アクセス権 metadata only access
アクセス権URI http://purl.org/coar/access_right/c_14cb
業績分類
値 学術雑誌論文
教員氏名 土屋, 博紀

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土屋, 博紀

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発行、発表雑誌等、又は発表学会等の名称
値 Anesthesiology Research and Practice
巻
値 Volume 2013, Article ID 297141, 18 pages
単著、共著の別
値 Collaboration
発行又は発表の年月
日付 2013-08
ISBN
値 doi: 10.1155/2013/297141
概要
値 Despite a long history in medical and dental application, the molecular mechanism and precise site of action are still arguable for local anesthetics. Their effects are considered to be induced by acting on functional proteins or on membrane lipids, or on both. Local anesthetics primarily interact with sodium channels embedded in cell membranes to reduce the excitability of nerve cells and cardiomyocytes or produce a malfunction of the cardiovascular system. However, the membrane protein-interacting theory cannot explain all of the pharmacological and toxicological features of local anesthetics. The administered drug molecules must diffuse through the lipid barriers of nerve sheaths and penetrate into or across the lipid bilayers of cell membranes to reach the acting site on transmembrane proteins. Amphiphilic local anesthetics interact hydrophobically and electrostatically with lipid bilayers and modify their physicochemical property, with the direct inhibition of membrane functions, and with the resultant alteration of the membrane lipid environments surrounding transmembrane proteins and the subsequent protein conformational change, leading to the inhibition of channel functions. We review recent studies on the interaction of local anesthetics with biomembranes consisting of phospholipids and cholesterol. Understanding the membrane interactivity of local anesthetics would provide novel insights into their anesthetic and cardiotoxic effects.
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