Synthesis and in vitro evaluation of 18F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET |
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| Authors: | Edward G Robins Yongjun Zhao Imtiaz Khan Anthony Wilson Sajinder K Luthra Erik Årstad |
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| Institution: | 1. GE Healthcare MDx Research, MRC Cyclotron Building, Hammersmith Hospital, London W12 0NN, United Kingdom;2. GE Healthcare MDx Research, The Grove Centre, Amersham HP7 9LL, United Kingdom |
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| Abstract: | Two S-18F]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-d-aspartate receptors (NMDARs) with positron emission tomography (PET). 18F]1 and 18F]10 were synthesized by 18F]fluoroethylation and 18F]fluoromethylation of the thiol precursor 6, respectively. 18F]1 is a promising candidate NMDAR PET tracer, with low nanomolar affinity for the NMDA PCP-site, high selectivity and moderate lipophilicity. |
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