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[~3H]-哌唑唪是肾上腺素受体分析中重要的α_1放射性配基,是心血管病理研究和药物选筛中不可缺少的工具。它以溴化哌唑嗪为前体,在催化剂存在下,与氚气反应4h制得,然后在液氮冷冻下回收未反应的氚气,过滤掉催化剂,用乙醇作溶剂反复冷冻干燥三次除去不稳定氚。除掉不稳定氛的产物用0.01mol/l HCl:乙醇=1:1(V/V)溶剂溶解即为最终产品。其比活度为386.2GBq/mmol,放化纯度为98％。为了选择合适的氚化条件,分别观察了不同反应时间,不同氚压及不同氚源丰度对反应产率的影响。
[~ 3H] -piperazole is an important α_1 radioligand in adrenergic receptor assays and is an indispensable tool in cardiovascular pathology and drug screening. The method comprises the following steps: taking prazosin bromide as a precursor, reacting with tritium gas for 4h under the presence of a catalyst, recovering unreacted tritium gas under liquid nitrogen freezing, filtering the catalyst, repeatedly freeze-drying three times with ethanol as a solvent, Unstable tritium. The product of the destabilization is dissolved in 0.01 mol / l HCl: ethanol = 1: 1 (V / V) solvent to obtain the final product. The specific activity of 386.2GBq / mmol, radiochemical purity of 98%. In order to select suitable tritiated conditions, the effects of different reaction time, different tritium pressure and different tritium source abundance on reaction yield were observed.