【摘要】 我们参考制备氚标记埃托芬的方法,对二氢埃托芬进行了氚标记,首次成功地制备了氚标记二氢埃托芬。同时,还成功地制备了一批高比度的氚标记埃托芬。更多还原

【Abstract】 Dihydroetorphine and etorphine are agonist of opiate receptor. In order to study the opiate receptor and analgesic cause, we prepared their tritium labelled compounds with high specific activity.15, 16-3H-dihydroetorphine and 15, 16-3H-etorphine can be prepared by catalytic reduction of 15, 16-didehydro-dihydroetorphine and 15, 16-didehydroetorphine. The former compounds had been synthesised with dihydroetorphine and etorphine by Leonard’s reaction respectively.The products were purified by thin layer chromatography (TLC).The radiochemical purities are 95% and the specific activities are 35 Oi/m mol (3H-DHE), 44 Ci/mmol (3H-E) respectively.The specific binding activity with opiate receptor was determined by radio receptor assay.更多还原