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High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMe

High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMe

  1. Gradient
    David E. Nichols, Stewart P. Frescasa, Benjamin R. Chemela, Kenneth S. Rehderb, Desong Zhongb and Anita H. Lewin


    Abstract

    The title compound ([3H]INBMeO) was prepared by an O,O-dimethylation reaction of a t-BOC protected diphenolic precursor using no carrier added tritiated iodomethane in DMF with K2CO3. Removal of the t-BOC protecting group and purification by HPLC afforded an overall yield of 43%, with a radiochemical purity of 99% and specific activity of 164 Ci/mmol. The new radioligand was suitable for labeling human 5-HT2A receptors in two heterologous cell lines and had about 20-fold higher affinity than [3H]ketanserin.

    The title compound 1 was prepared in 99% radiochemical purity at a specific activity of 160 Ci/mmol. It had a Kd of 0.1–0.15 nM in two different heterologous cell lines stably expressing the human serotonin 5-HT2A receptor.