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最近,Alberto等人报道了一种在低压(约105Pa)条件下制备水溶性的有机金属络合物[99mTc- (CO)3(OH2)3]+的方法.该络合物在水和空气中均比较稳定,且水配体很容易被其他的络合能力较强的 配体所取代,这使得羰基络合物可作为放射性药物应用于核医学.考虑到[99mTc(CO)3(OH2)3]+是一种+1 价的络合物,于是用六甲氧基异丁基异腈(MIBI)取代上述络合物中的3个水配体,制得了一种新的有机 锝络合物[99mTc(CO)3(MIBI)3]+,其放射化学产率可达85%,且具有较好的体外稳定性.由于该络合物与 已被广泛应用的心肌显像剂[99mTc(MIBI)6]+具有相似的结构,因此,期望[99mTc(CO)3(MIBI)3]+也能在心 肌中浓集,并可改善[99mTc(MIBI)6]+心/肝比值偏低的缺点.随后进行的小鼠体内生物分布实验表明,该 络合物的确能在心肌中浓集,且具有较高的心/肝比和与[99mTc(MIBI)6]+相当的心/血比,这使得其具有 成为心肌灌注显像剂的潜力.
Recently, Alberto et al. Reported a method for preparing a water-soluble organometallic complex [99mTc- (CO) 3 (OH2) 3] + at low pressure (about 105 Pa). The complex is relatively stable in both water and air and the water ligands are readily replaced by other ligands that are more complex, making the carbonyl complexes useful as a radiopharmaceutical in nuclear medicine. Taking into account that [99mTc (CO) 3 (OH2) 3] + is a +1-valent complex, thus replacing the three water ligands in the above complex with hexamethoxyisobutylisonitrile (MIBI), A novel organic technetium complex [99mTc (CO) 3 (MIBI) 3] + has a radiochemical yield of 85% and good in vitro stability. Since this complex has a similar structure to the widely used myocardial imaging agent [99mTc (MIBI) 6] +, it is expected that [99mTc (CO) 3 (MIBI) 3] + will also be concentrated in the myocardium , And can improve the shortcomings of [99mTc (MIBI) 6] + low cardiac / liver ratio. Subsequent in vivo biodistribution experiments in mice showed that the complex did indeed concentrate in the myocardium and had a high cardiac / hepatic ratio and a heart / blood ratio comparable to [99mTc (MIBI) 6] +, which Making it the potential to be a myocardial perfusion imaging agent.