Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System
AbstractAlthough agarwood has been used as a tranquilizer in Asian countries for hundreds of years, the underlying pharmacological basis is still unclear. This study investigated the sedative-hypnotic effect of agarwood essential oil (AEO) using locomotor activity and pentobarbital-induced sleeping assays in mice. Single (1-day) and multiple (7- and 14-days) administrations of 60 mg/kg AEO generated significant sedative effect on inhibiting locomotor activity and hypnotic effect on pentobarbital-induced sleeping in mice. Interestingly, prolonged AEO treatment did not result in obvious desensitization. Concoitant measurement of the levels of brain neurotransmitters using ultrafast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) indicated that AEO had no significant effect on the levels of glutamic acid (Glu) and γ-aminobutyric acid (GABA) in the brain. However, the sedative-hypnotic effects were blocked by the type A GABA (GABAA) receptor antagonists bicuculline and flumazenil. In addition, AEO significantly elevated the expression of GABAA receptor subunits and subtypes in the cerebral cortex. Furthermore, AEO increased chlorine ion (Cl−) influx through GABAA receptors in human neuroblastoma cells. These results together demonstrate that AEO exerts its sedative-hypnotic effects through regulating gene expression of GABAA receptors and potentiating GABAA receptor function. View Full-Text
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Wang, S.; Wang, C.; Peng, D.; Liu, X.; Wu, C.; Guo, P.; Wei, J. Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System. Molecules 2017, 22, 2190.
Wang S, Wang C, Peng D, Liu X, Wu C, Guo P, Wei J. Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System. Molecules. 2017; 22(12):2190.Chicago/Turabian Style
Wang, Shuai; Wang, Canhong; Peng, Deqian; Liu, Xinmin; Wu, Chongming; Guo, Peng; Wei, Jianhe. 2017. "Agarwood Essential Oil Displays Sedative-Hypnotic Effects through the GABAergic System." Molecules 22, no. 12: 2190.
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