Down-regulation of NR2B Receptors Contributes to Analgesic Effects of Gentiopicroside in Persistent Inflammatory Pain
Gentiopicroside is one of the secoiridoid compound isolated from Gentiana lutea. It exhibits analgesicactivities in the mice. The anterior cingulate cortex（ACC) is a f-orebrain structure known for its rolesin pain transmission and modulation. Painful stimuli potentiate the prefrontal synaptic transmissionand induce glutamate NMDA NR2Breceptor expression in the ACC. But little is known aboutGentiopicroside on the per-sistent inflammatory pain and chronic pain-induced synaptic transmissionchanges in the ACC. The present study was undertaken to investigate its analgesic activities andcentral synaptic modulation to the peripheral painful inflammation. Gentiopicrosideproducedsignificant analgesic effects against persistent inflammatory pain stimuli i-n mice. Systemicadministration of Gentiopicroside significantly reversed NR2B over-expression during the chronicphases of persistent inflammation caused by hind-paw ad-ministration of complete Freunds adjuvant(CFA) in mice. Whole-cell patch-clamp reco-rdings revealed that Gentiopicroside significantlyreduced NR2B receptors mediated p-ostsynaptic currents in the ACC. Our findings provide strongevidence that analgesiceffects of Gentiopicroside involve down-regulation of NR2B receptors in theACC to persistent inflammatory pain.
持续性疼痛 疼痛刺激 谷氨酸 突触调制
招明高
第四军医大学药学系
国内会议
长沙
英文
510-511
2008-07-25（万方平台首次上网日期，不代表论文的发表时间）