11C-NS14492 as a novel PET radioligand for imaging cerebral alpha7 nicotinic acetylcholine receptors: in vivo evaluation and drug occupancy measurements

Anders Ettrup, Jens D Mikkelsen, Szabolcs Lehel, Jacob Madsen, Elsebet Ø Nielsen, Mikael Palner, Daniel B Timmermann, Dan Peters, Gitte M Knudsen

56 Citationer (Scopus)

Abstract

Small-molecule α(7) nicotinic acetylcholine receptor (α(7)nAChR) agonists are currently validated for use as treatment for cognitive disturbances in schizophrenia and in Alzheimer disease. A suitable radiolabeled α(7)nAChR PET tracer would be important for in vivo quantification of α(7)nAChR binding in humans and to measure α(7)nAChR occupancy of α(7)nAChR drug candidates. Here, we present the radiosynthesis and in vivo evaluation of (11)C-NS14492 as a selective α(7)nAChR PET radioligand.
OriginalsprogEngelsk
TidsskriftJournal of Nuclear Medicine
Vol/bind52
Udgave nummer9
Sider (fra-til)1449-56
Antal sider8
ISSN0161-5505
DOI
StatusUdgivet - 2011

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