中国药理学与毒理学杂志2004，Vol.18Issue(5)：321-326,6.
神经肌肉接头前阻断剂川楝素抑制大鼠大脑皮层突触体谷氨酸释放
Inhibition of glutamate release from rat cerebral synaptosomes by a prejunctional blocker toosendanin
摘要
Abstract
AIM To elucidate the mechanism of the action of toosendanin(TSN), which may provide a new clue for understanding the basic processes involved in transmitter release. METHODS Nerve terminals (synaptosomes) from rat cerebral cortex were used as a test system to study the effects of TSN. They were isolated by discontinuous density gradient centrifugation. The secretogogues used to evoke Glu release included 50 mmol·L-1 KCl, 1.5 μmol·L-1 calcimycin and 7.5 mmol·L-1 4-aminopyridine (4-AP). Glu released from synaptosomes was determined by measuring the fluorescence of NADH produced in oxidative dehydrogenation of Glu. RESULTSTSN obviously inhibited the Glu release evoked by KCl depolarization in a concentration- and time-dependent manner. The effect mainly resulted from TSN-induced block of the Ca2+-dependent transmitter release. After TSN application the Glu release evoked by elevating intracellular free-Ca2+ concentration ([Ca2+]i) with calcimycin also significantly decreased. CONCLUSIONTSN inhibited the Glu release from central synapses and the effect was assumed to be related to TSN-induced depression in the Ca2+-sensitivity of release machinery.关键词
川楝素/大脑皮质/突触体/氨基酸神经递质/谷氨酸/神经递质调节剂/卡西霉素/4-氨基吡啶Key words
toosendanin/cerebral cortex/synaptosomes/amino acid neurotransmitters/glutamates/neurotransmitter agents/calcimycin/4-aminopyridine分类
医药卫生引用本文复制引用
许彤辉,施玉樑,任小梅,周建营..神经肌肉接头前阻断剂川楝素抑制大鼠大脑皮层突触体谷氨酸释放[J].中国药理学与毒理学杂志,2004,18(5):321-326,6.基金项目
国家重点基础研究规划项目(G1999054000) （G1999054000）
国家自然科学基金(39870249) （39870249）
国家自然科学基金(30170302) （30170302）
上海市基础研究重点项目(02JC14011) （02JC14011）
