T. Collier, J. O'Brien, R. Waterhouse
Sep 1, 1996
Citations
0
Influential Citations
40
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[ 18 F]-1-(3-Fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine has been prepared as a potential sigma-1 receptor ligand for PET. The unlabeled ligand was found to be selective in vitro for the sigma-1 receptor [Ki(σ 1 ) 4.3 nM] when tested in a variety of neuroreceptor binding assays. Furthermore, the ligand is selective for sigma-1 over sigma-2 receptors in vitro, having only moderate affinity for the sigma-2 receptor [Ki(σ 2 ) = 144 nM)]. The lipophilicity of the ligand (log P 7.5 = 2.8) is appropriate for good brain uptake and low non-specific binding. Radiofluorination was accomplished using nucleophilic fluorination methods using an alkylmesylate precursor and the specific activity of the product was >74,000 MBq/μmole. The average radiochemical chemical yield after purification was 62.3 ± 5.2% (56-70% EOB ; n = 5) and the radiochemical purity of the product was >99%. The average time of synthesis and purification was 80 minutes.