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The effect of caffeine on ion current induced inhibitory amino acid neurotransmitter, GABA and glycine. Single periaqueductal gray neuron was acutely dissociated and nystatin perforated patch clamp was performed under voltage clamping condition.1. Caffeine evoked outward current in PAG neuron dose dependent manner. 1mM of caffeine application had no response, but 3mM caffeine evoked about 32.5±8.539㎀ outward ion current and 10mM caffeine evoked about 215.46±19.04㎀ outward current.2. 10-2mM GABA activated Cl- current and recorded by inward current. Caffeine inhibited GABA activated Cl- current concentration dependent manner. 10-2mM of caffeine had no effect on 10-2mM of GABA response, but 10-1mM caffeine inhibited GABA activated Cl- current about 5.74±2.13%, 1mM caffeine inhibited about 17.25±2.70%, 10mM caffeine inhibited GABA response about 45.31±7.17%.These results suggest that inhibitory effect of caffeine on inhibitory amino acid, GABA, response causes excitation of CNS and this is the basic mechanism of increasing effect aerobic exercise performance by caffeine. 1) 대진대학교487-711 경기도 포천군 포천읍 선단리 산 11-111 1. Daejin UniversitySan11-1 Sundanri Pochungun Kyunggido 487-711 516-911 Korea