Abstract
Molecular imaging of brain structures by highly sensitive non-invasive techniques offers unique possibilities in the understanding of physiological and pathological processes in the central nervous system. In particular, the quantitative analysis by positron emission tomography (PET) of α7 nicotinic acetylcholine receptors (α7 nAChR), which are involved in different signalling pathways in the brain, is assumed to provide important information on the relation between receptor dysfunction and the pathogeneses of neuropsychiatric brain diseases, but the applicability of this imaging approach is still hampered due to insufficient imaging agents. This paper presents the recent efforts made to develop PET radiotracers targeting α7 nAChR as well as the current state of the evaluation of the most promising radiolabelled compounds in animal models and humans.
Keywords: drug design, molecular imaging, neurodegeneration, nicotine, orthosteric ligand, acetyl-choline, tomography, positron, radioligands, radiotracers
Current Drug Targets
Title:Development of Radioligands for the Imaging of α7 Nicotinic Acetylcholine Receptors with Positron Emission Tomography
Volume: 13 Issue: 5
Author(s): Peter Brust, Dan Peters, Winnie Deuther-Conrad
Affiliation:
Keywords: drug design, molecular imaging, neurodegeneration, nicotine, orthosteric ligand, acetyl-choline, tomography, positron, radioligands, radiotracers
Abstract: Molecular imaging of brain structures by highly sensitive non-invasive techniques offers unique possibilities in the understanding of physiological and pathological processes in the central nervous system. In particular, the quantitative analysis by positron emission tomography (PET) of α7 nicotinic acetylcholine receptors (α7 nAChR), which are involved in different signalling pathways in the brain, is assumed to provide important information on the relation between receptor dysfunction and the pathogeneses of neuropsychiatric brain diseases, but the applicability of this imaging approach is still hampered due to insufficient imaging agents. This paper presents the recent efforts made to develop PET radiotracers targeting α7 nAChR as well as the current state of the evaluation of the most promising radiolabelled compounds in animal models and humans.
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Peter Brust, Dan Peters, Winnie Deuther-Conrad , Development of Radioligands for the Imaging of α7 Nicotinic Acetylcholine Receptors with Positron Emission Tomography , Current Drug Targets 2012; 13 (5) . https://dx.doi.org/10.2174/138945012800398955
DOI https://dx.doi.org/10.2174/138945012800398955 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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