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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/BaSO_4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,[~3H]F-7302),其比放射性为59 Ci/mM,放化纯度为98％。[~3H]F-7302与小鼠脑内阿片受体的特异性结合在浓度为4.5×10~(-9)M时达到饱和,解离常数Kd=1.25×10~(-9)M,最大结合量B_(max)=93.08×10~(12)M/g蛋白,其特异性结合与非特异性结合比值达10～15。
In this paper, Pd (NO3) 3 was used as a precursor and N- (1- (p-bromophenacyl) -3-methyl-4-piperidinyl] With tritium gas halogen - tritium displacement, tritium reduction carbonyl reaction. The reaction product was purified by silica gel chromatography and quantitatively determined by methyl orange colorimetry to give N- {1- [beta] -hydroxy-beta-tritium- [beta] - (p- tritolyl) ethyl] Methyl-4-piperidinyl} propionanilide (IV, [~ 3H] F-7302) having a specific radioactivity of 59 Ci / mM and a radiochemical purity of 98%. The specific binding of [~ 3H] F-7302 to opioid receptors in mouse brain reached saturation at 4.5 × 10 ~ (-9) M with Kd = 1.25 × 10 ~ (-9) M, The maximum binding amount B max (max) = 93.08 × 10-12 M / g protein, the specific binding to non-specific binding ratio of 10-15.