Oxymatrine-carbenoxolone sodium inclusion compound induces antinociception and increases the expression of GABA(A)alpha1 receptors in mice.
Oxymatrine-carbenoxolone sodium inclusion compound induces antinociception and increases the expression of GABA(A)alpha1 receptors in mice.
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DOI：
10.1016/j.ejphar.2009.09.065
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发表时间：
2010-01
影响因子：
5
通讯作者：
Junjun Zhou;Guang Yang;Shaoju Jin;Lijun Tao;Jianqiang Yu;Yuan-xu Jiang
中科院分区：
文献类型：
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作者：
Junjun Zhou;Guang Yang;Shaoju Jin;Lijun Tao;Jianqiang Yu;Yuan-xu Jiang
氧化苦参碱-甘珀酸钠包合物（OCSIC）是一种新型镇痛药，但其镇痛效果及作用机制尚不清楚。本研究探讨了OCSIC的镇痛作用及其对中枢神经系统γ-氨基丁酸A型α1（GABAAα1）受体表达的可能影响。OCSIC的抗伤害作用进行了评估，在热和化学行为模型的伤害。采用热板实验、尾部浸泡实验、醋酸致腹部收缩实验和福尔马林致疼痛实验对ICR小鼠进行观察。腹膜内（i. p.）或脑室内（i. c. v.）。在所有情况下，OCSIC产生了显着的剂量依赖性镇痛作用。OCSIC（150 mg/kg）可增加GABAAα1受体阳性细胞的表达。这些结果提示OCSIC的抗伤害作用可能涉及中枢神经系统和外周神经系统。GABAA受体参与OCSIC的抗伤害效应，目前正在研究中。
Oxymatrine–carbenoxolone sodium inclusion compound (OCSIC) has been reported as a novel painkiller, but its effectiveness and mechanism remain unknown. This study investigated the analgesic effects of OCSIC and the possible alterations in the expression of γ-aminobutyric acid type A α1 (GABAAα1) receptors in the central nervous system caused by the compound. The antinociceptive action of the OCSIC was assessed in thermal and chemical behavioral models of nociception. The hot-plate test, tail immersion test, acetic acid-induced abdominal constriction and formalin-induced pain were used in ICR mice. OCSIC was administered intraperitoneally (i.p.) or intracerebroventricularly (i.c.v.). In all cases, OCSIC produced significant dose-dependent antinociceptive effects. In addition, OCSIC (150mg/kg) increased the expression of positive staining cells of GABAAα1 receptors. These results reveal that the antinociceptive effects of OCSIC may be involved in the central nervous system and the peripheral nervous system. The involvement of GABAAreceptors in the antinociceptive effect of OCSIC is now under investigation.