Ruyan M K, Bakan D A, Skinner R W, Newman C, Gross M D, Counsell R E
Department of Medicinal Chemistry, University of Michigan Medical School, Ann Arbor 48109, USA.
Nucl Med Biol. 1995 Jan;22(1):95-103. doi: 10.1016/0969-8051(94)e0067-s.
Using organozinc cross-coupling reactions, two radiolabeled analogs of 15-(p-iodophenyl) pentadecanoic acid (IPPA) have been designed and synthesized as potential scintigraphic imaging agents for the heart. Both 15-(4-iodophenyl)-tridecylglycidic acid and 15-(4-iodophenyl)-2-methylene pentadecanoic acid were synthesized and radioiodinated. In tissue biodistribution studies in rats, only the alpha-methylene derivative of IPPA displayed a consistently higher heart to blood ratio and a substantially lower degree of thyroid accumulation than did IPPA alone. With respect to a scintigraphic imaging efficacy, the alpha-methylene analog of IPPA and IPPA itself showed essentially equivalent cardiac imaging profiles in rabbits, with a slight extension in imaging time for the alpha-methylene analog of IPPA.
利用有机锌交叉偶联反应，设计并合成了两种15 -（对碘苯基）十五烷酸（IPPA）的放射性标记类似物，作为心脏潜在的闪烁成像剂。合成了15 -（4 -碘苯基）-十三烷基缩水甘油酸和15 -（4 -碘苯基）- 2 -亚甲基十五烷酸并进行放射性碘化。在大鼠组织生物分布研究中，与单独的IPPA相比，只有IPPA的α-亚甲基衍生物显示出始终较高的心脏与血液比值和显著较低的甲状腺蓄积程度。关于闪烁成像效果，IPPA的α-亚甲基类似物和IPPA本身在兔子中显示出基本等效的心脏成像轮廓，IPPA的α-亚甲基类似物的成像时间略有延长。
