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KMID : 0365819880280020159
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Journal of Pusan Medical College
1988 Volume.28 No. 2 p.159 ~ p.167
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Effect of Lidocaine on Na^(+)-dapendent ^(14)C-GABA Uptake in Rabbit Brain Cortical Synaptosome
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Abstract
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The effect of local anesthetic, lidocaine, on Na´-dependent "C-gamma-aminobutyric acid (GABA) uptake in the synaptosome of rabbit brain cortex was studied
1. Synaptosomal "C-GABA uptake was stimulated by the presence of Na´ in incubation medium but not by the presence of other cations.
2. Lidocaine inhibited reversibly Na´-dependent "C-GABA uptake in a dose-dependent manner, but not affected Na´-independent uptake. Fifty percent of inhibition was shown at 4 x 10-´M.
3. Lidocaine inhibited synaptosomal´Na-K-ATPase activity in a dose-dependent manner at concentrations above lOjM.
Ouabain(1 mM) and harmaline(1 mM) also inhibited synaptosomal Na´-dependent "C-GABA uptake in 55. 5±3.87% and 36.7±2.83% respectively, and the effect of lidocaine was additive when treated together with these drugs.
It is suggested that lidocaine inhibits Na´-dependent GABA transport in rabbit brain cortical synaptosome affecting both the inhibition of Na´-pump and the reduction of the affinity, and the mobility of GABA transporter by nonspecific deterioration of synaptoscmal membrane.
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