EFFECTS OF LOCAL ANESTHETICS ON MONOAMINE OXIDASE, AND THEIR MEMBRANE EFFECTS
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概要
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The effects of various local anesthetics on rat brain and liver monoamine oxidase (MAO) and their antihemolytic and local anesthetic effects were studied. All local anesthetics tested at 1×10<SUP>-7</SUP> M to 1×10<SUP>-3</SUP> M inhibited MAO activity in rat liver mitochondria with 5-hydroxytryptamine (5-HT) as substrate. The order of potency was tetracaine>procaine> dibucaine>lidocaine>prilocaine. Tetracaine and procaine inhibited 5-HT oxidation much more than β-phenylethylamine (PEA) oxidation. Dibucaine inhibited PEA oxidation as much as 5-HT oxidation. Inhibition of MAO by local anesthetics other than dibucaine was reversible. Tetracaine and procaine inhibited 5-HT oxidation competitively, whereas dibucaine inhibited it non-competitively. Antihemolytic effects were observed with dibucaine and tetracaine at concentrations of 6 × 10<SUP>-5</SUP> M and 1×10<SUP>-4</SUP> M, respectively. The order of surface anesthetic potencies was dibucaine>tetracaine> prilocaine>lidocaine>procaine. These results suggest that the inhibition of MAO activities by local anesthetics depends on both electrostatic and hydrophobic interactions between these drugs and enzyme-associated phospholipids or the hydrophobic regions of proteins.
- 社団法人 日本薬理学会の論文
著者
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KAMIJO Kazuya
Department of Pharmacology, School of Medicine, Showa University
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Sakamoto Koji
Department Of Pharmacology School Of Medicine Showa University
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Yasuhara Hajime
Department Of Neonatal Intensive Care Unit Nara Prefectural Hospital
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WADA Ikuho
Department of Pharmacology, School of Medicine, Showa University
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