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.

该α -氨基-3-羟基-5-甲基-4-异恶唑丙酸受体（的AMPARs）属于家族离子型跨膜受体谷氨酸（离子型谷氨酸受体），其在神经系统疾病和神经变性疾病的病理学牵连的。受最近开发的AMPAR的正变构调节剂的启发，4-环丙基-7-（3-甲氧基苯氧基）-3,4-二氢-2 H-苯并[ e ] [1]，[2]，[4]噻二嗪1 1-二氧化物（16 ; EC ₅₀ = 2.0 nM），我们为N保护的酚类前体13设计了一条新的合成路线，并有效地对PET配体进行了放射性标记[ ¹¹ C] AMPA-1905（[ ¹¹ C]16）在高放射化学产率和高摩尔活性中使用改良的一锅两步策略。进行了初步的体内评估，以研究[ ¹¹ C] 16作为AMPAR成像的潜在PET探针的适用性。