反式曲马朵及反式氧去甲基曲马朵对映体在大鼠中枢神经系统的分布

目的：研究反式曲马朵（trans-T)及其活性代谢产物反式氧去甲基曲马朵（M1）对映体的中枢神经系统分布。方法：大鼠ip单剂量的盐酸trans-T或M1后，采用高效毛细管电泳（HPCE）法测定血清和不同脑组织中trans-T及M1对映体的浓度，脑组织包括脑脊液、大脑皮层、纹状体、下丘脑、小脑、延髓。结果：大鼠ip盐酸trans-T后，在血清及所有测试脑组织中，（＋）－trans-T的浓度均高于（－）－trans-T的浓度；在所有测试脑组织中，（＋）－M1的浓度均低于（－）－M1的浓度；trans-T和（＋）－M1对映体的浓度以大脑皮层中最高，脑脊液中最低。大鼠ip M1后，在血清及所有测试脑组织中，（＋）－M1的浓度均高于（－）－M1的浓度；M1对映体的浓度以大脑皮层中最高，脑脊液中最低。结论：在血清和不同脑组织中，trans-T及M1对映体的浓度是有区别的；trans-T及M1在中枢神经系统的分布具有立体选择性；大鼠ip M1与trans-T后，M1在中枢神经系统分布的立体选择性是不同的。

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

AIM: To investigate the distribution of the enantiomers of trans-tramadol (trans-T) and its active metabolite, frans-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 electro-phoresis (HPCE) method was used to determine the concentrations of enantiomers of trans-T and Ml 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 ( ) -Ml were lower than those of ( - )-Ml in the all tested brain tissues; The concentrations of the enantiomers of trans-T and Ml were the highest in the CC, the lowest in theCF. After ip M1, the concentrations of ( )-M1 were higher than those of ( - )-Ml in the serum and all tested brain tissues; The concentrations of the enantiomers of Ml 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 Ml 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.