Bier D, Dutschka K, Knust E J
Nuklearchemie und Radiopharmazie-Klinik für Nuklearmedizin Universitätsklinikum, Essen, Germany.
Nucl Med Biol. 1996 Apr;23(3):373-6. doi: 10.1016/0969-8051(96)00018-2.
By variation of reaction parameters iodination of 3-(9,10-didehydro-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea (lisuride) was performed with the radiohalogen [123I]iodine (t1/2 = 13.3 h). For comparative experiments and stability studies the beta(-)-emitting radioisotope [131I]iodine (t1/2 = 8.04 d) was also used. Reaction occurs at the activated position 2 of the molecule, thus leading to [123I]3-(9,10-didehydro-2-iodo-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea ([123I]2-iodo-lisuride, [123I]ILIS) or the analogous [131I]iodine-labeled compound, respectively. Electrophilic radioactive species were generated by oxidation of no-carrier-added (n.c.a.) iodide with IODOGEN (1,3,4,6-tetrachloro-3 alpha,6 alpha-diphenylglycouril) fixed on the glass wall of the reaction vial prior to iodination. After optimization of reaction parameters [123I]2-iodo-lisuride after HPLC-purification was obtained with radiochemical yields of 70 +/- 5% and a radiochemical purity of > 97%. In n.c.a. syntheses, specific activities of the product were in the range between 4440 and 7400 GBq/mumol (120-200 Ci/mumol) corresponding to 50-85% of the theoretical value.
通过改变反应参数，用放射性卤素[123I]碘（半衰期t1/2 = 13.3小时）对3-(9,10-二脱氢-6-甲基-8α-麦角灵基)-1,1-二乙基脲（利苏瑞）进行碘化反应。为了进行对比实验和稳定性研究，还使用了发射β(-)射线的放射性同位素[131I]碘（半衰期t1/2 = 8.04天）。反应发生在分子的活性2位，从而分别生成[123I]3-(9,10-二脱氢-2-碘-6-甲基-8α-麦角灵基)-1,1-二乙基脲（[123I]2-碘-利苏瑞，[123I]ILIS）或类似的[131I]碘标记化合物。在碘化反应前，通过用固定在反应瓶玻璃壁上的碘代甘脲（1,3,4,6-四氯-3α,6α-二苯基脲）氧化无载体添加（n.c.a.）碘化物来生成亲电放射性物质。在优化反应参数后，经高效液相色谱（HPLC）纯化得到[123I]2-碘-利苏瑞，其放射化学产率为70±5%，放射化学纯度>97%。在无载体添加合成中，产物的比活度在4440至7400 GBq/μmol（120 - 200 Ci/μmol）范围内，相当于理论值的50 - 85%。
