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Objective To observe carbenoxolone sodium Oxymatrine inclusion complexes (Oxymatrine-carbenoxolone sodium inclusion compound, OCSIC), central inhibition and to explore its central inhibition mechanisms. Behavioral Pharmacology the methods observed OCSIC of threshold dose and subthreshold dose of sodium pentobarbital (Pentobarbital, PENT) hypnotic effects of the impact on the ability and endurance of mice active and passive activities coordination. GABA synthesis and release of the inhibitor, γ-aminobutyric acid (Gamma aminobutyric acid, GABA), GABA receptor agonists and antagonists, GABA transporter 1 (GABA transporter-1, GAT-1) inhibitor Tools drugs Research OCSIC central inhibition and analysis of its mechanism of action. Immunohistochemical method (SABC) to measured OCSIC cerebral cortex of mice, the hippocampus and brainstem reticular GAT-1 and PKC-Υ immunoreactive nerve cells, analysis OCSIC central inhibition and brain GAT-1 , PKC-Υ. 1. OCSIC100, 50 and 25 mg / kg can cause a decrease in spontaneous activity (P lt; 0.01) inhibition rates were 86.7%, 85.6%, 17.2%; PENT sleep latency were reduced by 61.2%, 49.0% , 36.7% (P lt; 0.01), sleep duration extension of 379.8%, 146.2% and 132.2% (P lt; 0.01, P lt; 0.05), and significantly strengthen the subthreshold dose PENT the hypnotic effect (P lt ; 0.05). The prompt OCSIC obvious central inhibition. 2. OCSIC100 mg / kg against GABA synthesis and release inhibitor 3 - mercaptopropionic acid (3-Mercaptopropionic acid ,3-MP)-induced convulsive effect (P lt; 0.01), seizure latency increased to 7.6 from 2.8 ± 0.44 s ± 1.34 s (P lt; 0.01); subliminal dose OCSIC subliminal dose GABA or 3 - piperidinecarboxylate (Ethyl nipecotate, EN) combination could be synergistic reduction of spontaneous activity, spontaneous activity rates were down 78.78% and 47.04% (P lt; 0.01); OCSIC100 mg / kg in the cerebral cortex of mice can reduce GAT-1 immunoreactive number of nerve cells in the hippocampus and brainstem reticular (P lt; 0.01). Step OCSIC central inhibition associated with GABA neurotransmission, role by increasing GABA synthesis and release, and reduce the GABA transporter. 3 threshold dose of OCSIC with subthreshold doses of muscimol (Muscimol, MUS) or baclofen (Baclofen, BAC) combination could be synergistic reduction of spontaneous activity, independent activity rate decreased by 57.69% and 19.12% (P lt ; 0.01); OCSIC100 mg / kg with a threshold anti-convulsive dose stability (Diazepam, DZ) combination can Duikang purse peony alkali (Bicuculine, BIC) and India Anti own toxins (Picrotoxin, PTX) induced convulsive effect (P lt; 0.01) but not against kainic acid (kainic acid, KA), NMDA-induced convulsion. Central inhibition and activate GABA prompted OCSIC nerve receptors, no direct relationship with the KA, NMDA receptor. 4. OCSIC100 mg / kg enables mouse cerebral cortex, hippocampus, and brainstem reticular structure the PKC-Υ immunoreactive reduce the number of nerve cells (P lt; 0.01). Prompted OCSIC central inhibition of PKC-Υ. The the conclusion OCSIC obvious central inhibition, its site of action involves the cerebral cortex, hippocampus and brainstem reticular uplink system the, OCSIC central inhibition mechanism may can with GABA neurotransmitter, by increasing the synthesis and release of GABA, reducing GABA transporter play a role, its mechanism is also excited GABA receptor, reducing the cerebral cortex, hippocampus and brainstem reticular GAT-1, PKC-Υ expression.
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