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为研究~(125)I-AIBZM 与多巴胺 D_2受体的结合特性,通过二步合成反应制得左旋碘标记前体 ABZM。在室温 pH值3条件下,氯胺 T 法制得~(125)I-AIBZM。以大鼠纹状体膜蛋白作为多巴胺 D_2受体制剂,用放射配基结合分析法研究~(125)I-AIBZM 的结合特性。结果:碘标记前体 ABZM 白色粉状的熔点为135℃～137℃,并经~1H NMR 确证结构。~(125)I-AIBZM 标记率为90%,放化纯度为95%,比活度为80TBq/mmol。Scatchard 分析其平衡解离常数为3.41×10~(-11)mol/L,最大结合容量为20.60±0.74fmol/mg 蛋白质。因此,~(125)I-AIBZM 是一个结合力强的多巴胺 D_2受体配基,作为潜在的神经受体显像剂有进一步研究价值。
In order to study the binding properties of ~ (125) I-AIBZM to dopamine D_2 receptors, ABZM, a precursor of iodinated iodine, was synthesized by a two-step synthesis reaction. Under the condition of pH 3 at room temperature, chloramine T method was used to produce ~ (125) I-AIBZM. Rat striatal membrane protein was used as a dopamine D2 receptor preparation, and the binding properties of ~ (125) I-AIBZM were studied by radioligand binding assay. Results: The melting point of the iodine labeled precursor ABZM was 135 ℃ ~ 137 ℃. The structure was confirmed by ~ 1H NMR. The labeling rate of ~ (125) I-AIBZM was 90%, the radiochemical purity was 95% and the specific activity was 80TBq / mmol. Scatchard analysis of the equilibrium dissociation constant of 3.41 × 10 ~ (-11) mol / L, the maximum binding capacity of 20.60 ± 0.74fmol / mg protein. Thus, ~ (125) I-AIBZM is a well-binding dopamine D 2 receptor ligand that is of further value as a potential neuroreceptor imaging agent.