Abstract: Schizandrol A is one of the active constituents isolated from the ethanol extract of dried fruit of Schizandra chinensis Baill (Fructus Schizandra). It was found to have neuroleptic and anticonvulsive effects in animals. A method of high specificity using TLC for the determination of Schizandrol A in biological, specimens was developed and used in the study of the metabolism of the drug in rats and the distrubution in various areas of rat brain.After oral administration Schizandrol A was found to be readily, absorbed from the gastro-intestinal tract (t_1/2=58 min). The bloodlevel of Schizandrol A following iv injection showed a biphasic decline as a function of time, the distribution phase and the elimination phase. The pharmacokinetic parameters were as follows:t_1/2α=1.44 min, t_1/2β=42.14 min, K₁₀=0.08/min, K₁₂=0.32/min, K₂₁=0.10/min, V_c=0.75 L/kg, V_d=3.60 L/kg. Schizandrol A was detectable in urine one hour after oral administration About 0.35% of the dose was recovered from urine within 26 hours. Five minutes after iv injection highest levels of Schizandrol A was found in the lung, moderate in liver, heart, brain and kidneys, and low in ileum and spleen. These results indicate that Schizandrol A was distributed widely in the body and eliminated rapidly.The distribution of Schizandrol A in various areas of the brain was as follows:highest levels was found in hypothalamus, striatum and hippocampus, moderate indiencephalon and lower stem, and low in cerebral Cortex and cerebelum. The different levels in various regions of the brain might be relevant to the neuroleptic and cataleptic effects of Schizandrol A.