✦ LIBER ✦

Synthesis of 1-(trans-[123I]Iodopropen-2-yl)-4-(4-cyanophenoxy-methyl)piperidine: A selective sigma receptor radioligand for SPECT

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

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 604 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199603)38:3<215::aid-jlcr834>3.0.co;2-f

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✦ Synopsis

1 -( truns-[ 1Z3I ]Iodopropen-3-yl)-4-(4-cyanophenoxymethyl)pipidine has been prepared as a novel sigma receptor ligand for SPECT. This ligand was found lo be selective in v i m for the sigma receptor site (&(a) = 21.7 nM) when tested in a variety of neuroreceptor binding assays. The lipophilicity of this ligand (log P7.5 = 3.36) is appropriate for good brain uptake and relatively low non-specific binding. Radioiodination was accomplished using classical electrophilic iododestannylation methods and specific activity of the purified product was >2100 mCi/pmole. Radiochemical yields were 60-80% EOS and radiochemical purities were >99%. The avcrage time of synthesis and purification was 35 minutes.

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