Recent progress in allosteric modulators for GluN2A subunit and development of GluN2A-selective nuclear imaging probes.
Yingfang HeLinjing MuSimon M AmetameyRoger SchibliPublished in: Journal of labelled compounds & radiopharmaceuticals (2020)
N-methyl-D-aspartate (NMDA) receptors play key roles in physiology by regulating the synaptic plasticity and the cellular mechanism involved in learning and memory. The GluN2A subunit is the most abundant expression of NMDA receptors in mature brain, and its dysfunction has been implicated in various neurological disorders. However, the function of GluN2A subunit in physiological and pathological conditions is not yet completely unveil due to the lack of subunit-selective ligands, including specific positron emission tomography (PET)/single photon emission computed tomography (SPECT) imaging probes. In this review, recent progresses in understanding its pathophysiological role, the structure-activity relationship, and the postulated mechanisms of novel GluN2A ligands as well as status of molecular imaging probes for PET are summarized.
Keyphrases
- positron emission tomography
- computed tomography
- small molecule
- pet ct
- fluorescence imaging
- high resolution
- living cells
- pet imaging
- single molecule
- structure activity relationship
- protein kinase
- magnetic resonance imaging
- dual energy
- poor prognosis
- white matter
- contrast enhanced
- multiple sclerosis
- image quality
- oxidative stress
- cerebral ischemia
- long non coding rna
- blood brain barrier
- mass spectrometry
- binding protein