The pharmacokinetics of piceatannol, pinosylvin and rhapontigenin were characterized in male Sprague-Dawley rats after single intravenous doses of 10 mg kg−1 of each stilbene. Serial blood samples were collected via a catheter inserted into the right jugular vein and plasma samples were analysed for the selected stilbenes concentrations using reverse phase HPLC methods. After an acute intravenous dose of piceatannol, plasma AUC, urine t½, CL and Vd were 8.48 ± 2.48 μgh mL−1, 19.88 ± 5.66 h, 2.13 ± 0.92 Lh−1 kg−1 and 10.76 ± 2.88 Lkg−1 (mean ± s.e.m.), respectively. The acute intravenous dose of pinosylvin yielded the plasma AUC, urine t ½, CL and Vd values of 5.23 ± 1.20 μgh mL−1, 13.13 ± 2.05 h, 1.84 ± 0.44 Lh−1 kg−1 and 2.29 ± 0.56 Lkg−1 (mean ± s.e.m.), respectively. Rhapontigenin intravenous dosing yielded the plasma AUC, urine t½, CL and Vd values of 8.39 ±0.10 μgh mL−1, 25.31 ± 1.46 h, 1.18 ± 0.035 Lh−1 kg−1 and 11.05 ± 0.17 Lkg−1 (mean ± s.e.m.), respectively. Each stilbene was extensively glucuronidated. These stilbenes were predominantly eliminated via non-urinary routes. All three stilbenes were highly distributed into tissues and were highly extracted by the liver. The detectable plasma half-lives of these xenobiotics appear to be relatively short. However, utilizing urinary concentration-time data, much longer elimination half-lives were evident. The estimates of oral bioavailability characterize these stilbenes as poorly bioavailable compounds.