Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 11, Pages 6116-6123Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.04.050
Keywords
radioligand; 5-HT2A receptor; receptor binding
Funding
- NIDA NIH HHS [DA02189, R01 DA002189, R56 DA002189, R01 DA002189-27] Funding Source: Medline
- NIMH NIH HHS [N01-MH-32005, N01MH32005] Funding Source: Medline
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The title compound ([H-3]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 [H-3] ketanserin. (C) 2008 Elsevier Ltd. All rights reserved.
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