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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

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

Volume 16, Issue 16, 2016

Page: [1830 - 1842] Pages: 13

DOI: 10.2174/1568026616666160315142457

Price: $65


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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