A new brain perfusion imaging agent: [I-123]HIPDM:N,N,N'-trimethyl-N'-[2-hydroxy-3-methyl-5-iodobenzyl]-1,3-propanediamine.
A new brain perfusion imaging agent: [I-123]HIPDM:N,N,N'-trimethyl-N'-[2-hydroxy-3-methyl-5-iodobenzyl]-1,3-propanediamine.
复制标题
一种新型脑灌注显像剂：[I-123]HIPDM:N,N,N-三甲基-N-[2-羟基-3-甲基-5-碘苄基]-1,3-丙二胺。
作者：
H. Kung;K. Tramposch;M. Blau
根据pH值漂移机理，研制了一种新的脑显像剂I-124 HIPDM（N，N，N '-trimethyl-N'-[2-hydroxy-3-methyl-5-[123 I]iodobenzyl]-1，3-propanediamine）。该试剂可以通过适合于常规临床使用的简单交换反应来制备。理化参数、分配系数与pH值曲线、蛋白结合率以及大鼠中的生物分布与I-123 IMP（N-异丙基-p-碘苯丙胺）非常相似。静脉注射后，在动物中发现高脑摄取。在大鼠和猴中，脑放射性至少持续1小时。大鼠脑切片中的区域分布似乎反映了区域灌注。结合单光子发射断层扫描（SPECT），这种代理人可以提供有用的信息，在人类局部脑灌注。
Based on the pH-shift mechanism, a new brain imaging agent I-124 HIPDM (N,N,N'-trimethyl-N'-[2-hydroxy-3-methyl-5-[123I]iodobenzyl]-1,3-propanediamine ) has been developed. This agent can be prepared by a simple exchange reaction suitable for routine clinical use. The physicochemical parameters, partition coefficient vs. pH profile, and protein binding, as well as biodistribution in rats, were very similar to those of I-123 IMP (N-isopropyl-p-iodoamphetamine). High brain uptake was found in animals after i.v. injection. The brain radioactivity persists for at least 1 hr in rats and monkeys. Regional distribution in sections of rat brain appeared to reflect regional perfusion. In conjunction with single-photon emission tomography (SPECT), this agent may provide useful information on local cerebral perfusion in humans.