214209-96-8Relevant articles and documents
Radiosynthesis and preliminary evaluation of 11C-labeled 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-benzo[e] [1,2,4] thiadiazine 1,1-dioxide for PET imaging AMPA receptors
Chen, Jiahui,Chen, Zhen,Collier, Lee,Deng, Xiaoyun,Fu, Hualong,Gan, Jiefeng,Gong, Jian,Liang, Steven H.,Rong, Jian,Shang, Jingjie,Shao, Tuo,Sun, Jiyun,Wang, Lu,Xu, Hao
, (2020/01/31)
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-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide (16; EC50 = 2.0 nM), we designed a new synthetic route for N-protected phenolic precursor 13 and efficiently radiolabeled a PET ligand [11C]AMPA-1905 ([11C]16) using a modified one-pot two-step strategy in high radiochemical yield and high molar activity. Preliminary in vivo evaluation was carried out to investigate the suitability of [11C]16 as a potential PET probe for AMPAR imaging.
Benzothiadiazine compound, application thereof and positron drug of AMPAR
-
, (2020/03/02)
The invention relates to a benzothiadiazine compound, application thereof and a positron drug of AMPAR (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor). The structure of the benzothiadiazine compound is shown as the specification, wherein R is selected from one of Br, Cl, F, I and the groups shown as the specification. A marked benzothiadiazine compound prepared by taking the above benzothiadiazine compound as a precursor has high standard uptake value and high specificity to AMPAR.
Cycloalkylated benzothiadiazines, a process for their preparation and pharmaceutical compostions containing them
-
Page/Page column 13, (2010/02/17)
Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group,R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.