Abstract Z)-N-tert-butyl-1-(5-((((E)-3-(3,4-dihydroxyphenyl)acryloyl)oxy)methyl)-3,6-dimethylpyrazin-2-yl) methani mine oxide (CT-011), a novel derivative of tetramethylpyrazine (TMP) was designed and synthesized in our laboratory, can effectively scavenge free radicals and protect nerve cells. A developed and validated high performance liquid chromatography (HPLC) was used to evaluate the pharmacokinetics of CT-011, the limit of quantitywas0.02 μg/mL. Within the intravenous dose of CT-011 range from 10 to 90 mg/kg in rats, the plasma concentration decreased rapidly, and the half-life of terminal elimination ranges from 22.833 to 42.257 min. The concentration of CT-011 in lung tissue was significantly higher than that in other tissues, suggesting that lung tissue may be its main target organ. The main metabolites of CT-011 in rats were caffeic acid and 2-N-tert-butyl nitrone-5-hydroxymethyl-3,6-dimethylpyrazine (5-OH-TBN) in vivo and in vitro. The results provide basic information for the pharmacodynamic study and further clinical study of CT-011.
Keywords Pharmacokinetic, Metabolism, Quantitative determination, Plasma concentration, Tissues distribution.