Arteaga de Murphy C, Ferro-Flores G, Villanueva-Sanchez O, Murphy-Stack E, Pedraza-López M, Meléndez-Alafort L, Molina-Trinidad E
Departamento de Medicina Nuclear, Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, Vasco de Quiroga #15, Tlalpan, Mexico D.F. 14000, Mexico.
Int J Pharm. 2002 Feb 21;233(1-2):29-34. doi: 10.1016/s0378-5173(01)00922-x.
Infarct-avid radiopharmaceuticals are necessary for rapid and timely diagnosis of acute myocardial infarction. The animal model used to produce infarction implies artery ligation but chemical induction can be easily obtained with isoproterenol. A new infarct-avid radiopharmaceutical based on glucaric acid was prepared in the hospital radiopharmacy of the INCMNSZ. 99mTc-glucarate was easy to prepare, stable for 96 h and was used to study its biodistribution in rats with isoproterenol-induced acute myocardial infarction. Histological studies demonstrated that the rats developed an infarct 18 h after isoproterenol administration. The rat biodistribution studies showed a rapid blood clearance via the kidneys. Thirty minutes after 99mTc-glucarate administration the standardised heart uptake value S(h)UV was 4.7 in infarcted rat heart which is six times more than in normal rats. ROIs drawn over the gamma camera images showed a ratio of 4.4. The high image quality suggests that high contrast images can be obtained in humans and the 96 h stability makes it an ideal agent to detect, in patients, early cardiac infarction.
梗死灶摄取放射性药物对于急性心肌梗死的快速及时诊断至关重要。用于产生梗死的动物模型意味着动脉结扎,但使用异丙肾上腺素可轻松实现化学诱导。一种基于葡萄糖二酸的新型梗死灶摄取放射性药物在国家核医学与分子影像科学研究所医院的放射性药房制备。99mTc-葡萄糖二酸盐易于制备,可稳定96小时,并用于研究其在异丙肾上腺素诱导的急性心肌梗死大鼠中的生物分布。组织学研究表明,大鼠在给予异丙肾上腺素18小时后出现梗死。大鼠生物分布研究显示,药物通过肾脏快速清除。给予99mTc-葡萄糖二酸盐30分钟后,梗死大鼠心脏的标准化心脏摄取值S(h)UV为4.7,是正常大鼠的6倍。在γ相机图像上绘制的感兴趣区显示比值为4.4。高图像质量表明在人体中可获得高对比度图像,96小时的稳定性使其成为检测患者早期心肌梗死的理想药物。