Title of article :
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): A high-affinity 5-HT2A receptor-selective agonist radioligand Original Research Article
Author/Authors :
David E. Nichols، نويسنده , , Stewart P. Frescas، نويسنده , , Benjamin R. Chemel، نويسنده , , Kenneth S. Rehder، نويسنده , , Desong Zhong، نويسنده , , Anita H. Lewin، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
8
From page :
6116
To page :
6123
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.
Keywords :
Receptor binding , 5-HT2A receptor , Radioligand
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2008
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1304416
Link To Document :
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