Schisandrin B exerts hypnotic effects in PCPA-treated rats by increasing hypothalamic 5-HT and γ-aminobutyric acid levels.

Schisandrin B (SchB) is one of the primary active components of (Turcz.) Baill., a traditional Chinese herb that has been used to treat insomnia for hundreds of years. Our previous studies revealed that SchB exerts sedative and hypnotic effects, increasing the content of γ-aminobutyric acid (GABA) and the expression of its receptors in the brain tissues of rats. 5-hydroxytryptamine (5-HT) is another important neurotransmitter involved in sleep regulation, although, to the best of our knowledge, there are no reports of its association with SchB. Therefore, the present study aimed to determine whether the hypnotic effect of SchB was partly due to alterations in the expression of 5-HT. The results indicated that SchB reduced sleep latency and increased sleep duration in parachlorophenylalanine (PCPA)-induced rats with insomnia by increasing 5-HT and 5-hydroxyindoleacetic acid, and upregulating the expression of the 5-HT receptor 1A in the hypothalamus. SchB also increased the ratio of GABA to glutamic acid and the activity of glutamic acid decarboxylase, decreased the activity of GABA transaminase, and upregulated the expression of GABA receptor α1 and GABA receptor γ2 in the rat hypothalamus. These results suggested that SchB improved PCPA-induced insomnia in rats, and its effects may be associated with the regulation of GABA and 5-HT levels in the hypothalamus.