✦ LIBER ✦

Synthesis of a selective sigma receptor radioligand for SPECT: [123I]-1-(2-hydroxyethyl)-4-(4-iodophenoxymethyl)piperidine

✍ Scribed by Rikki N. Waterhouse; T. Lee Collier; J. C. O'Brien

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 507 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199607)38:7<595::aid-jlcr882>3.0.co;2-a

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✦ Synopsis

123I]-1-(2-Hydroxyethyl)-4-(4-iodophenoxymethy~)piperidine has been prepared as a novel sigma receptor radioligand for tumour imaging by SPECT. This ligand was found to be selective in vitro for the sigma-1 receptor (Ki = 2.3 nM) when tested in a variety of neuroreceptor binding assays. The lipophilicity of this ligand is appropriate for crossing the bloodhain barrier (log P7.5 = 4.0). Radioiodination was accomplished by no-carrier-added iododestannylation using chloramine-T in acetic acid. The specific activity of the radiotracer >10,000 mCilpmole. The radiochemical yield was 63-77% EOS and the radiochemical purity was >99%.

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