University of Missouri Research Reactor, University of Missouri, Columbia, MO, 65211, USA.
Laboratory of Neuroimaging, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, MD, 20892-1013, USA.
Eur J Med Chem. 2022 Dec 5;243:114764. doi: 10.1016/j.ejmech.2022.114764. Epub 2022 Sep 17.
As one of the nine subtypes of adrenergic receptors (ARs) in the brain, α2C-ARs play essential roles in emotion and memory, and are implicated in neuropsychiatric disorders, including depression, Alzheimer's disease, substance use disorder, and schizophrenia. A recently developed α2C-AR specific positron emission tomography (PET) radiotracer, [C]ORM-13070, showed promise for imaging α2C-ARs in the brain. Herein, we prepared highly potent C-11 labeled benzo-1,4-dioxane derivatives and compared them with [C]ORM-13070, aiming to improve the specific binding signal, as evaluated by in vivo rodent brain PET imaging.© 2022 Elsevier Inc. All rights reserved.
作为大脑中九种肾上腺素能受体 (AR) 亚型之一，α2C-AR 在情绪和记忆中发挥着重要作用，并与神经精神疾病有关，包括抑郁症、阿尔茨海默病、物质使用障碍和精神分裂症。最近开发的一种 α2C-AR 特异性正电子发射断层扫描 (PET) 放射性示踪剂 [C]ORM-13070，为脑内 α2C-AR 成像提供了希望。在此，我们制备了高活性的 C-11 标记苯并-1,4-二恶烷衍生物，并将其与 [C]ORM-13070 进行了比较，旨在通过体内啮齿动物脑 PET 成像来提高特异性结合信号。© 2022 年 Elsevier Inc. 保留所有权利。
