论文部分内容阅读
为了找到适合123I标记的5-羟色胺(5-HT1A)受体显像剂,合成了4-三正丁基锡-N-[2-[1-(2-甲氧基苯基)]-1-哌嗪基]乙基-N-2-吡啶基-苯甲酰胺(MPPBu3Sn,标记前体),并采用双氧水标记法进行131I标记,得到标记物131I-MPPI,标记率大于90%,放化纯大于99%。初步动物实验结果显示,131I-MPPI在大鼠海马中摄取最多,30 min时,海马与小脑的摄取率比值为2.90,说明131I-MPPI浓集在海马中,与5-HT1A受体在脑中的分布一致;放射自显影结果显示,在注射8-OH-DPAT后,海马(CA3区)与小脑的光密度比值从13.98±0.87降至1.96±0.46,与阻断前差异显著,说明131I-MPPI与5-HT1A受体结合具有特异性;注射后5 min和120 min,甲状腺的摄取率分别为(0.069±0.020)%和(0.128±0.026)%,表明脱碘是其主要代谢途径;131I-MPPI对5-HT1A受体具有高度亲和性和特异性,可作为筛选其他化合物对5-HT1A受体亲和大小的工具药。
In order to find a serotonin (5-HT1A) receptor imaging agent suitable for 123I labeling, 4-tri-n-butyltin-N- [2- [1- (2-methoxyphenyl) (MPPBu3Sn, labeled precursor), and labeled with 131I by hydrogen peroxide method to obtain 131I-MPPI labeled product with a labeling rate of more than 90% 99%. Preliminary animal experiments showed that 131I-MPPI uptake in the hippocampus of rats up to 30 min, the hippocampal and cerebellar uptake ratio was 2.90, indicating that 131I-MPPI concentration in the hippocampus, and 5-HT1A receptor in the brain The results of autoradiography showed that after 8-OH-DPAT injection, the optical density ratio of hippocampus (CA3 area) to cerebellum decreased from 13.98 ± 0.87 to 1.96 ± 0.46, which was significantly different from the pre-blocking value, indicating that 131I- MPPI was specific to 5-HT1A receptor. The uptake rates of thyroid at 5 min and 120 min after injection were (0.069 ± 0.020)% and (0.128 ± 0.026)%, respectively, indicating that deiodination was the main metabolic pathway; 131I -MPPI has a high affinity and specificity for the 5-HT1A receptor and can be used as a tool to screen the affinity of other compounds for the 5-HT1A receptor.