Rafii H, Chalon S, Ombetta J E, Frangin Y, Garreau L, Dognon A M, Lena I, Bodard S, Vilar M P, Besnard J C
INSERM U316, Laboratoire de Biophysique Médicale et Pharmaceutique, UFR des Sciences Pharmaceutiques, Tours, France.
Nucl Med Biol. 1995 Jul;22(5):617-23. doi: 10.1016/0969-8051(94)00144-9.
We described the radiosynthesis of an analog of Ro 16-6491, [125I]N-(2-aminoethyl)-4-iodobenzamide, for SPECT exploration of the monoamine oxidase B (MAO-B) in human brain. The radiolabelling was carried out by nucleophilic exchange of the brominated precursor at solid-state phase in presence of ammonium sulphate. The radiochemical purity of radioiodinated product was higher than 95%. In comparison with Ro 16-6491, the in vitro studies showed a good selectivity of stable N-(2-aminoethyl)-4-iodobenzamide for MAO-B but a slightly lower affinity. Biodistribution studies in the rat showed a high and selective uptake of this compound in the pineal gland 1 h after i.v. injection. The cerebral uptake was low, but the coupling of [125I]N-(2-aminoethyl)-4-iodobenzamide with a lipophilic radical to enhance the passage through the blood-brain barrier can be envisaged.
我们描述了一种Ro 16-6491类似物[125I]N-(2-氨基乙基)-4-碘苯甲酰胺的放射性合成方法，用于单光子发射计算机断层显像（SPECT）研究人脑中的单胺氧化酶B（MAO-B）。放射性标记是在硫酸铵存在下，通过溴化前体在固相阶段的亲核交换进行的。放射性碘化产物的放射化学纯度高于95%。与Ro 16-6491相比，体外研究表明稳定的N-(2-氨基乙基)-4-碘苯甲酰胺对MAO-B具有良好的选择性，但亲和力略低。在大鼠体内进行的生物分布研究表明，静脉注射1小时后，该化合物在松果体中具有高选择性摄取。脑摄取较低，但可以设想将[125I]N-(2-氨基乙基)-4-碘苯甲酰胺与亲脂性基团偶联以增强其通过血脑屏障的能力。
