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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging

Author(s): Victor W. Pike

Volume 23, Issue 18, 2016

Page: [1818 - 1869] Pages: 52

DOI: 10.2174/0929867323666160418114826

Price: $65


The development of reversibly binding radioligands for imaging brain proteins in vivo, such as enzymes, neurotransmitter transporters, receptors and ion channels, with positron emission tomography (PET) is keenly sought for biomedical studies of neuropsychiatric disorders and for drug discovery and development, but is recognized as being highly challenging at the medicinal chemistry level. This article aims to compile and discuss the main considerations to be taken into account by chemists embarking on programs of radioligand development for PET imaging of brain protein targets.

Keywords: PET, radioligand, molecular imaging, positron-emitter, carbon-11, fluorine-18, efflux transporter, blood-brain barrier.

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