Radiosynthesis and Preliminary Evaluation of C-labeled 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2-benzo[] [1,2,4] Thiadiazine 1,1-dioxide for PET Imaging AMPA Receptors

Overview

Journal Tetrahedron Lett

Publisher Elsevier

Specialty Chemistry

Date 2020 Mar 11

PMID 32153306

Citations 4

Authors

Jiahui Chen

Jiefeng Gan

Jiyun Sun

Zhen Chen

Hualong Fu

Jian Rong

Xiaoyun Deng

Jingjie Shang

Jian Gong

Tuo Shao

Lee Collier

Lu Wang

Hao Xu

Steven H Liang

Affiliations

Soon will be listed here.

Abstract

The α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) belong to the family of ionotropic transmembrane receptors for glutamate (iGluRs) that are implicated in the pathology of neurological disorders and neurodegenerative diseases. Inspired by a recently developed positive allosteric modulator of AMPARs, 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2-benzo[ ][1,2,4]thiadiazine 1,1-dioxide (; EC = 2.0 nM), we designed a new synthetic route for -protected phenolic precursor and efficiently radiolabeled a PET ligand [C] ([C]) using a modified one-pot two-step strategy in high radiochemical yield and high molar activity. Preliminary evaluation was carried out to investigate the suitability of [C] as a potential PET probe for AMPAR imaging.

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