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正电子发射断层扫描和单光子发射计算机断层扫描示踪剂用于谷氨酸受体。

PET and SPECT tracers for glutamate receptors.

机构信息

Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University, New York, NY 10032, USA.

出版信息

Drug Discov Today. 2013 Feb;18(3-4):173-84. doi: 10.1016/j.drudis.2012.10.004. Epub 2012 Oct 22.

Abstract

Radioligands for PET imaging of glutamate receptors will have the potential for studying neurological and neuropsychiatric disorders and their diagnosis and therapeutic intervention. Glutamate is the major excitatory neurotransmitter in the brain and is implicated in the pathophysiology of many neurodegenerative and neuropsychiatric disorders. Glutamate and its receptors are potential targets in the treatment of these disorders. Glutamate signaling is mediated through ionotropic and metabotropic receptors. The abundant concentration of these receptors can facilitate their in vivo quantification using positron emission tomography (PET). Glutamate receptors are a potentially important set of targets for monitoring disease progression, for evaluating the effect of therapy and for new treatment development based on the quantification of receptor occupancy. Here, we review the PET and single-photon emission computed tomography (SPECT) radioligands that have been developed for imaging glutamate receptors in living brain.

摘要

用于正电子发射断层扫描(PET)成像谷氨酸受体的配体将有可能用于研究神经和神经精神疾病及其诊断和治疗干预。谷氨酸是大脑中的主要兴奋性神经递质,与许多神经退行性和神经精神疾病的病理生理学有关。谷氨酸及其受体是这些疾病治疗的潜在靶点。谷氨酸信号通过离子型和代谢型受体介导。这些受体的丰富浓度可以使用正电子发射断层扫描(PET)方便地对其进行体内定量。谷氨酸受体是一组潜在的重要靶点,可用于监测疾病进展,评估治疗效果,并根据受体占有率的定量进行新的治疗开发。在这里,我们综述了用于活体脑内成像谷氨酸受体的 PET 和单光子发射计算机断层扫描(SPECT)配体。

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