Synthesis and Preclinical Evaluation of 2-(2-Furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-

详细信息    查看全文

• 作者：Xiaoyun Zhou ; Shivashankar Khanapur ; Anja P. Huizing ; Rolf Zijlma ; Marianne Schepers ; Rudi A. J. O. Dierckx ; Aren van Waarde ; Erik F. J. de Vries ; Philip H. Elsinga
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：November 13, 2014
• 年：2014
• 卷：57
• 期：21
• 页码：9204-9210
• 全文大小：306K
• ISSN：1520-4804

文摘

2-(2-Furanyl)-7-[2-[4-[4-(2-[p>11p>C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine [p>11p>C]-3 ([p>11p>C]Preladenant) was developed for mapping cerebral adenosine A_2A receptors (A_2ARs) with PET. The tracer was synthesized in high specific activity and purity. Tissue distribution was studied by PET imaging, ex vivo biodistribution (BD), and in vitro autoradiography (ARG) experiments. Regional brain uptake of [p>11p>C]-3 was consistent with known A_2ARs distribution, with highest uptake in striatum. The results indicate that [p>11p>C]-3 has favorable brain kinetics and exhibits suitable characteristics as an A_2AR PET tracer.