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Purpose: To investigate the therapeutic effects of Jiaotai pill (JTP) on rats with insomnia induced by pchlorophenylalanine (PCPA). Methods: Rats with PCPA-induced insomnia were divided into 5 groups ( n = 10), made up of control group, positive treatment group (estazolam 0.1 mg/kg), and 3 JTP treatment groups (0.6, 1.2 and 2.4 g/kg). Another group of 10 rats were treated as normal group. Rats in normal and control groups were treated with normal saline (10 mL/kg). After 14 days of drug treatment, the rats were injected intraperitoneally with sodium pentobarbital (45 mg/kg) and thereafter, latent period and sleeping time were recorded, while contents of γ-aminobutyric acid (GABA) and glutamic acid (Glu) in hypothalamus were determined by high performance liquid chromatography (HPLC). Furthermore, the expressions of glutamate decarboxylase 65 (GAD-65), glutamate decarboxylase 67 (GAD-67), GABAaminotransferase (GABA)-T, anti-GABA transporter 1 (GAT)-1, anti-GABA transporter (GAT)-3, and GABA receptors (GABA-A and GABA-B) in the hypothalamus were analyzed by western blotting assay. Results: The results showed that JTP (0.6, 1.2 and 2.4 g/kg) significantly shortened latent period and prolonged sleeping time ( p < 0.01). JTP also increased GABA level ( p < 0.01), but decreased Glu contents of the rat hypothalamus ( p < 0.01). Western blotting data indicate that JTP significantly upregulated the levels of GAD-65 ( p < 0.01), GAD-67 ( p < 0.05), GAT-1 ( p < 0.01), GAT-3 ( p < 0.01), GABA-A ( p < 0.01) and GABA-B ( p < 0.01), while the level of GABA-T was down-regulated. Conclusion: The results demonstrate that JTP possesses significant sedative effects on insomnia in rats, most probably through a mechanism involving GABA signal pathway. Keywords: Jiaotai pill, Insomnia, GABA, Glutamate, Estazolam, GABA signal pathway

Therapeutic effects of Jiaotai pill on rat insomnia via regulation of GABA signal pathway