Vaidyanathan G, Affleck D J, Zalutsky M R
Department of Radiology, Duke University Medical Center, Durham, North Carolina 27710.
J Med Chem. 1994 Oct 14;37(21):3655-62. doi: 10.1021/jm00047a022.
The aims of this investigation were to develop a no-carrier-added (nca) synthesis of (4-[18F]-fluoro-3-iodobenzyl)guanidine ([18F]FIBG) and to evaluate its potential as an MIBG analogue useful for positron emission tomography. [18F]FIBG was prepared in four steps starting from 4-cyano-2-iodo-N,N,N-trimethylanilinium trifluoromethanesulfonate in 5% decay-corrected radiochemical yield in a total synthesis time of 130 min. The specific activity was more than 1500 Ci per mmol. In vitro binding studies showed that the percent binding of [18F]FIBG to SK-N-SH human neuroblastoma cells remained constant over a 3-log activity range and was similar to that of nca [131I]MIBG. Specific and high uptake of FIBG was also seen in mouse heart and adrenals. The in vitro and in vivo properties of [18F]FIBG suggest that this compound may be a useful positron-emitting analogue of MIBG.
本研究的目的是开发一种无载体添加（nca）合成（4-[¹⁸F]氟-3-碘苄基）胍（[¹⁸F]FIBG）的方法，并评估其作为用于正电子发射断层扫描的MIBG类似物的潜力。[¹⁸F]FIBG从4-氰基-2-碘-N，N，N-三甲基苯胺三氟甲磺酸盐开始分四步制备，衰变校正后的放射化学产率为5%，总合成时间为130分钟。比活度超过1500居里/毫摩尔。体外结合研究表明，[¹⁸F]FIBG与SK-N-SH人神经母细胞瘤细胞的结合百分比在3个对数活性范围内保持恒定，并且与nca [¹³¹I]MIBG相似。在小鼠心脏和肾上腺中也观察到FIBG的特异性和高摄取。[¹⁸F]FIBG的体外和体内特性表明，该化合物可能是一种有用的MIBG正电子发射类似物。
