Sedative-
hypnotic medications, including
benzodiazepines and non-
benzodiazepines, are usually prescribed for the insomniac patients; however, the addiction, dependence and adverse effects of those medications have drawn much attention. In contrast,
suanzaorentang, a traditional Chinese herb remedy, has been efficiently used for
insomnia relief in China, although its mechanism remains unclear. This study was designed to further elucidate the underlying mechanism of
suanzaorentang on sleep regulation. One ingredient of
suanzaorentang,
zizyphi spinosi semen, exhibits binding affinity for
serotonin (5-hydroxytryptamine, 5-HT) receptors, 5-HT(1A) and 5-HT(2), and for
GABA receptors. Our previous results have implicated that
GABA(A) receptors, but not
GABA(B), mediate
suanzaorentang-induced sleep alteration. In current study we further elucidated the involvement of
serotonin. We found that high dose of
suanzaorentang (4 g/kg/2 ml) significantly increased non-rapid eye movement sleep (NREMS) when comparing to that obtained after administering
starch placebo, although placebo at dose of 4 g/kg also enhanced NREMS comparing with that obtained from baseline recording. Rapid eye movement sleep (REMS) was not altered. Administration of either 5-HT(1A) antagonist (NAN-190), 5-HT(2) antagonist (
ketanserin) or 5-HT(3 )antagonist (3-(4-Allylpiperazin-1-yl)-2-quinoxalinecarbonitrile) blocked
suanzaorentang-induced NREMS increase. These results implicate the
hypnotic effect of
suanzaorentang and its effects may be mediated through serotonergic activation, in addition to GABAergic system.