Original Article

Distribution of enantiomers of trans-tramadol and trans-O-demethyltramadol in central nervous system of rats

Authors: Hui-Chen Liu, Na Wang, Chang-Suo Liu, Yu-Qin Hu, Jian-Fang Liu, Yan-Ning Hou

Abstract

Aim: To investigate the distribution of the enantiomers of trans-tramadol (trans-T) and its active metabolite, trans-O-demethyltramadol (M1), in the central nervous system (CNS).
Methods: After a single ip dose of trans-T hydrochloride or M1, the rats were killed by decapitation. A high performance capillary electrophoresis (HPCE) method was used to determine the concentrations of enantiomers of trans-T and M1 in the serum and different brain tissues, including cerebrospinal fluid (CF), cerebral cortex (CC), corpus striatum (CS), hypothalamus (HY), cerebellum (CE), and medulla oblongata (MO).
Results: After ip trans-T hydrochloride, the concentrations of (+)-trans-T were higher than those of (-)-trans-T in the serum and all tested brain tissues; The concentrations of (+)-M1 were lower than those of (-)-M1 in the all tested brain tissues; The concentrations of the enantiomers of trans-T and M1 were the highest in the CC, the lowest in the CF. After ip M1, the concentrations of (+)-M1 were higher than those of (-)-M1 in the serum and all tested brain tissues; The concentrations of the enantiomers of M1 were the highest in the CC, the lowest in the CF.
Conclusion: The concentrations of the enantiomers of trans-T and M1 varied in the serum and different brain tissues. The distribution of trans-T and M1 in the CNS of rats was stereoselective. The stereoselectivity in the distribution of M1 after M1 injection was different with that after trans-T injection.
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