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  • Title: [Transportation of the enantiomers of trans tramadol and O-demethyltramadol across blood-brain barrier].
    Author: Liu HC, Hu YQ, Liu JF, Wang N, Hou YN.
    Journal: Yao Xue Xue Bao; 2001 Sep; 36(9):644-7. PubMed ID: 12580098.
    Abstract:
    AIM: To investigate the transportation of the enantiomers of trans tramadol (trans T) and its active metabolite, O-demethyltramadol (M1) across blood-brain barrier. METHODS: Rats were sacrificed by femoral artery bleeding 1 h after i.p. administration of trans T hydrochloride, 16.7 mg.kg-1 or 50.0 mg.kg-1. Blood, cerebrospinal fluid and cerebral cortex were taken out. The enantiomers of trans T and M1 were analyzed by high performance capillary electrophoresis (HPCE). RESULTS: Among the three tissues, the concentration of each enantiomer of trans T and M1 was the highest in the cerebral cortex, and the lowest in the cerebrospinal fluid. In the serum, the concentration of (+)-trans T was higher than that of (-)-trans T, and the concentrations of the enantiomers of M1 were similar. In the cerebrospinal fluid and cerebral cortex, the concentration of (+)-trans T was higher than that of (-)-trans T, and the concentrations of (+)-M1 was lower than that of (-)-M1. CONCLUSION: The transportation across blood-brain barrier of the enantiomers of trans T and M1 was stereoselective. In the brain tissues, the concentrations of (+)-trans T and (-)-M1 were higher than those of their enantiomers.
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