摘要
完成了一种七步化学合成得到前体螺环哌啶醇的方法,并用H2O2-冰醋酸氧化标记法和TLC纸层析法分离合成了溴(~77Br)代螺环哌啶醇。标记率为92%,放射化学产率为78%,产品的放射化学纯度>95%。并对该放射性药物在小白鼠脑内的吸收分布作了初步研究,结果表明在大脑纹状体中的摄取率可高出小脑6倍.
his report describes the routine method for producing spiroperidol by seven steps of chemical synthesis. Br-p-bromospiroperidol was prepared by reacting 77Br, H2O2 and spiroperidol in glacial acetic acid. The purity of the product was checked by TLC. The labelling rate was 92% and the overall radiochemical yield was 78% with radiochemical purity of 95%. The in vivo distribution of 77Br-p-bromospiroperidol in the mouse brain was studied. It was shown that the uptake of 77Br-p-bromospiroperidol in striatum was six times higher than that in cerebellum.
出处
《核技术》
CAS
CSCD
北大核心
1994年第4期233-237,共5页
Nuclear Techniques
关键词
神经受体
显像剂
螺环哌啶醇
溴77
Neuroreceptor imaging agent, Dopamine D_2 receptor, Spiroperidol