A liquid chromatography/tandem mass spectrometry (LC/MS/MS) method was developed and validated for the determination and pharmacokinetics of danshensu in rat plasma samples using ferulic acid as internal standard (IS). The plasma samples were treated by liquid-liquid extraction, and the analyses were determined using electrospray negative ionization mass spectrometry in selected reaction monitoring (SRM) mode. The signal intensity of the m/z 196.8 --> 134.8 transition of danshensu was found to relate linearly to danshensu concentrations in the plasma from 5-500 ng/mL. The lower limit of quantification (LLOQ) as determined by the LC/MS/MS method amounted to 5 ng/mL. The intra- and inter-day precision was below 10.82%, and the accuracy was between -3.51% and +11.92%. The validated LC/MS/MS method was applied to a pharmacokinetic study in which danshen extract (containing 40 mg/g danshensu) was administered orally to rats at a single dose of 200 mg/kg in 2% water.