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

…, TL Collier, JC O'Brien

Index: Waterhouse; Collier; O'Brien Journal of Labelled Compounds and Radiopharmaceuticals, 1996 , vol. 38, # 3 p. 215 - 226

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Citation Number: 12

Abstract

Abstract 1-(trans-[123 I] Iodopropen-2-yl)-4-(4-cyanophenoxymethyl) piperidine has been prepared as a novel sigma receptor ligand for SPECT. This ligand was found to be selective in vitro for the sigma receptor site (Ki (σ)= 21.7 nM) when tested in a variety of neuroreceptor binding assays. The lipophilicity of this ligand (log P 7.5= 3.36) is appropriate for good brain uptake and relatively low non-specific binding. Radioiodination was accomplished using ...