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

Author(s): Alina Kassenbrock, Neil Vasdev, Steven H. Liang

Journal Name: Current Topics in Medicinal Chemistry

Volume 16 , Issue 16 , 2016

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Graphical Abstract:


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.

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

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Article Details

Year: 2016
Page: [1830 - 1842]
Pages: 13
DOI: 10.2174/1568026616666160315142457
Price: $65

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PDF: 53
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