周德和, 倪崇虎, 吴益芝, 李志毅, 刘景芝, 唐国忠, 赵夏令. 氚标记强效镇痛剂N-1-(β-羟基-β-苯乙基)-3-甲基-4-哌啶基-N-丙酰苯胺的制备以及与阿片受体的结合试验J. 药学学报, 1982, 17(9): 658-662.
引用本文: 周德和, 倪崇虎, 吴益芝, 李志毅, 刘景芝, 唐国忠, 赵夏令. 氚标记强效镇痛剂N-1-(β-羟基-β-苯乙基)-3-甲基-4-哌啶基-N-丙酰苯胺的制备以及与阿片受体的结合试验J. 药学学报, 1982, 17(9): 658-662.
ZHOU De-he, NI Chong-hu, WU Yi-zhi, LI Zhi-yi, LIU Jing-zhi~, TANG Guo-zhong~ , ZHAO Xia-ling, . PREPARATION OF 3H-LABELLED N-1-(β-HYDROXY β-PHENYLETHYL)-3-METHYL-4-PIPERIDYL-N-PHENYLPROPIONAMIDE AND STUDIES OF ITS BINDING WITH OPLATE RECEPTORS OF MOUSE BRAINJ. Acta Pharmaceutica Sinica, 1982, 17(9): 658-662.
Citation: ZHOU De-he, NI Chong-hu, WU Yi-zhi, LI Zhi-yi, LIU Jing-zhi~, TANG Guo-zhong~ , ZHAO Xia-ling, . PREPARATION OF 3H-LABELLED N-1-(β-HYDROXY β-PHENYLETHYL)-3-METHYL-4-PIPERIDYL-N-PHENYLPROPIONAMIDE AND STUDIES OF ITS BINDING WITH OPLATE RECEPTORS OF MOUSE BRAINJ. Acta Pharmaceutica Sinica, 1982, 17(9): 658-662.

氚标记强效镇痛剂N-1-(β-羟基-β-苯乙基)-3-甲基-4-哌啶基-N-丙酰苯胺的制备以及与阿片受体的结合试验

PREPARATION OF 3H-LABELLED N-1-(β-HYDROXY β-PHENYLETHYL)-3-METHYL-4-PIPERIDYL-N-PHENYLPROPIONAMIDE AND STUDIES OF ITS BINDING WITH OPLATE RECEPTORS OF MOUSE BRAIN

  • 摘要: 本文报道以N-1-(对-溴苯甲酰甲基)-3-甲基-4-哌啶基-N-丙酰苯胺(Ⅲ)为前体,以PdO/BaSO4作催化剂,用氚气进行卤—氚置换,氚化还原羰基的反应。反应产物经硅胶纸层析纯化后,用甲基橙比色法定量测定,得到N-1-β-羟基-β-氚-β-(对-氚苯基)乙基-3-甲基-4-哌啶基-N-丙酰苯胺(Ⅳ,3HF-7302),其比放射性为59 Ci/mM,放化纯度为98%。3HF-7302与小鼠脑内阿片受体的特异性结合在浓度为4.5×10-9M时达到饱和,解离常数Kd=1.25×10-9M,最大结合量Bmax=93.08×1012M/g蛋白,其特异性结合与非特异性结合比值达10~15。

     

    Abstract: A new potent narcotic analgesic, N-1-(β-hydroxy β-phenylethyl)-3-methyl-4-piperidyl-N-phenylpropionamide (simply named as F-7302) was labelled by tritiumhalogen exchange and catalytic reduction of N-1-(p-bromo-benzoyl methyl)-3-methyl-4-piperidyl-N-phenylpropionamide with tritium gas, using PdO/BaSO4 as catalyst, removal of labile tritium by treating with alcohol, and final purification with silica-gel paper chromatography. Methyl orange was employed for the quantitative determination of 3H F-7302. The specific radioactivity was 59 ci/mM, and the radiochemical purity was 98%.3H F-7302 binding experiments with opiate receptors of mouse brain showed a high affinity and specificity. The saturation concentration for the stereospecific binding of 3HF-7302 was 4.5×10-9M. and the dissociation constant was 1.25×10-9M.The retio of specific/nonspecific binding was 10~15.

     

/

返回文章
返回