Dannals R F, Burns H D, Marzilli L G, Trageser T C, Wagner H N
J Pharm Sci. 1981 Apr;70(4):439-42. doi: 10.1002/jps.2600700425.
Two radioiodinated analogs of benzoylcholine were investigated as possible myocardial-imaging agents. O-([2-125I]Iodobenzoyl)-choline and N-([2-125I]iodobenzoyl)cholamine were prepared by nucleophilic substitution of sodium [125I]iodide for stable iodine in O-(N,N]dimethylaminoethyl)-2-iodobenzoate and N-(N',N'-dimethylaminoethyl)-2-iodobenzamide, respectively, and by methylation with methyl iodide. The in vivo distribution of each compound in mice was determined as a function of time. Favorable heart-to-blood and heart-to-lung ratios were obtained with N-([2-125I]iodobenzoyl)cholamine.
研究了两种苯甲酰胆碱的放射性碘化类似物作为潜在心肌显像剂的可能性。通过用[125I]碘化钠对O-(N,N-二甲基氨基乙基)-2-碘苯甲酸酯和N-(N',N'-二甲基氨基乙基)-2-碘苯甲酰胺中的稳定碘进行亲核取代,分别制备了O-([2-125I]碘苯甲酰基)-胆碱和N-([2-125I]碘苯甲酰基)胆胺,并用碘甲烷进行甲基化。测定了每种化合物在小鼠体内的分布随时间的变化情况。N-([2-125I]碘苯甲酰基)胆胺获得了良好的心脏与血液以及心脏与肺的比率。