The Korean Journal of Pharmacology (대한약리학회지)
- Volume 24 Issue 1
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- Pages.17-29
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- 1988
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- 0377-9459(pISSN)
Effect of Lidocaine on the Release, Receptor Binding and Uptake of Amino Acid Neurotransmitters In vitro
Lidocaine이 아미노산 신경전도물질의 유리, 수용체 결합, 및 섭취에 미치는 효과에 관한 시험관내 실험에 관한 연구
- Oh, An-Min (Department of Pharmacology, Osaka Dental University) ;
- Cheong, Dong-Kyun (Department of Pharmacology and Dental Therapeutics, College of Dentistry, Seoul National University) ;
- Mori, Masakazu (Department of Pharmacology, Osaka Dental University)
- Published : 1988.06.30
Abstract
The author examined the effects of lidocaine on the veratrine-or potassium-induced release of neurotransmitters to determine the possible role of amino acid neurotransmitters in lidocaine-induced convulsion. The examined transmitters were gamma-aminobutyric acid (GABA), aspartic acid, glutamic acid and norepinephrine which are released from the synaptosomes. Furthermore, the effects of lidocaine on the binding to receptors and synaptosomal uptake of the two transmitters, GABA and glutamic acid, were determined in crude synaptic membranes and synaptosomes. In addition, the effects of propranolol, norepinephrine and serotonin on the release of amino acid neurotransmitters were also examined. The veratrine-induced release of GABA was most severely inhibited by lidocaine and propranolol, while norepinephrine and serotonin reduced the release of aspartic acid and glutamic acid more than the GABA release. Generally the potassium-induced release was much more resistant to the lidocaine action than the veratrine-induced release. Among the neurotransmitters examined, the aspartic acid release was most prone to the lidocaine action, while the GABA release was most resistant. Concentrations of lidocaine below 1 mM did not significantly change the GABA and glutamic acid receptor binding and uptake. These results indicate that the blocking of sodium channels by lidocaine can result in the selective depression of the GABA release. This may result in unlimited excitation of the central nervous system.
Lidocaine 투여에 의한 전신경련의 작용기전을 추구하고자 흰쥐의 전체뇌를 또는 선조체, 해마, 및 중뇌를 부위별로 적출하여 synaptosomes를 마련하고