Journal of labelled compounds and radiopharmaceuticals p. 595 - 605 (1996)
Update date:2022-09-26
Topics:
Waterhouse, Rikki N.
Collier, T. Lee
O'Brien
[123I]-1-(2-Hydroxyethyl)-4-(4-iodophenoxymethyl)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 blood/brain 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 mCi/μmole. The radiochemical yield was 63-77% EOS and the radiochemical purity was >99%.
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