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Bioorg Med Chem. 2008 Jun 1;16(11):6116-23. doi: 10.1016/j.bmc.2008.04.050. Epub 2008 Apr 25.

High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.

Author information

1
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 1333 Robert E. Heine Pharmacy Building, West Lafayette, IN 47907, USA. drdave@pharmacy.purdue.edu

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 K(2)CO(3). 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 164Ci/mmol. The new radioligand was suitable for labeling human 5-HT(2A) receptors in two heterologous cell lines and had about 20-fold higher affinity than [(3)H]ketanserin.

PMID:
18468904
PMCID:
PMC2719953
DOI:
10.1016/j.bmc.2008.04.050
[Indexed for MEDLINE]
Free PMC Article

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