Journal of Life Science (생명과학회지)
- Volume 2 Issue 2
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- Pages.97-107
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- 1992
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- 1225-9918(pISSN)
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- 2287-3406(eISSN)
Molecular Mechanism of Action of Local Anesthetics: A Review
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Yun, Il
(Departments of Dental Pharmacology and Biophysics, College of Dentistry, Pusan National University) ;
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Kang, Jung-Sook
(Departments of Oral Biochemistru and Molecular Biology, College of Dentistry, Pusan National University)
- Published : 1992.04.01
Abstract
Strichartz and Richie have suggested that the mechanism of sodium donductance block of local anesthetics involves their interaction with a specific binding site within the sodium channel. However, there is evidence that local anesthetics can interact electrostatically with membrane proteins as well as membrane lipids. Whether or not all actions of local anesthetics are mediated by common site remains unclear. Thus, it can not be ruled out that local anesthetics concurrently interact with neuronal membrane lipids since sodium channels were found to be tightly associated with membrane lipids through covalent or noncovalent bonds. In summary, it is strongly postulated that local anesthetics, in addition to their direct interaction with sodium channels, concurrently interact with membrane lipids, fluidize the membrane, and thus induce conformational changes of sodium channels, which are known to be tightly associated with membrane lipids.
비록 국소마취제가 신경세포막 당단백질중의 하나인 sodium channel과의 직접적인 상호작용에 의하여 그 특유의 국소마취제를 나타낸다고 할지라도 신경세포막의 골격을 형성하고 있는 지질과 국소마취제와의 상호작용을 분자적 국소마취제 작용기전을 설명함에 있어 배제할 수는 없다. 왜냐하면 sodium channel은 지질과의 공유 또는 비공유결합을 통해 단단하게 결합되어 있기 때문이다. 따라서 국소마취제가 직접 sodium channel과 결합, 상호작용하여 Na+의 유입을 차단할 뿐만 아니라 직접 지질의 측방 및 회전확산 운동을 증가시킴으로써 간접적으로 sodium channel의 conformational change가 유발되어 Na+의 유입이 차단되는 등의 복합적인 기전에 의하여 그 특유의 국소마취작용이 나타나는 것이다.
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