180847-22-7Relevant academic research and scientific papers
Synthesis of a selective sigma receptor radioligand for SPECT: [123I]-1-(2-Hydroxyethyl)-4-(4-iodophenoxymethyl)piperidine
Waterhouse, Rikki N.,Collier, T. Lee,O'Brien
, p. 595 - 605 (1996)
[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%.
