~F]-1-(3-Fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine has been prepared as a potential sigma-I receptor ligand for PET. The unlabeled ligand was found to be selective in vitro for the sigma-I receptor [Ki(crl) = 4.3 nM] when tested in a variety of neuroreceptor binding assays. Furthermore, the l
Synthesis of N1-3-[18F]fluoropropyl-N4-2-([3,4-dichlorophenyl]ethyl)piperazine, a high affinity ligand for sigma receptor
✍ Scribed by Dale O. Kiesewetter; Brian de Costa
- Publisher
- John Wiley and Sons
- Year
- 1993
- Tongue
- French
- Weight
- 275 KB
- Volume
- 33
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
The radiochemical synthesis of the high affinity, selective sigma receptor ligand, N^1^‐3‐[^18^F]Fluoropropyl‐N^4^‐2‐([3,4‐dichlorophenyl]ethyl)piperazine, is reported. The labeled compound is prepared by fluoride displacement on a bismethanesulfonate salt of the propyl methanesulfonyloxy precursor. The product is isolated by first passage through a BONDELUT‐SI and subsequently HPLC in high radiochemical and chemical purity with a decay corrected radiochemical yield of 49 ± 9%.
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