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Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors

[ Vol. 16 , Issue. 16 ]


Alina Kassenbrock, Neil Vasdev and Steven H. Liang   Pages 1830 - 1842 ( 13 )


Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-D-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.


Positron Emission Tomography, Ion Channel, γ-Aminobutyric Acid-Benzodiazapine Receptor, Nicotinic Acetylcholine Receptor, N-Methyl-D-Aspartate Receptor.


Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Massachusetts General Hospital and Harvard Medical School, Boston, MA, USA.

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