TY - DATA T1 - Synthesis and Evaluation of Dimeric Derivatives of 5-HT2A Receptor (5-HT2AR) Antagonist M-100907 PY - 2016/02/22 AU - Matthew J. Shashack AU - Kathryn A. Cunningham AU - Patricia K. Seitz AU - Andrew McGinnis AU - Thressa D. Smith AU - Cheryl S. Watson AU - Scott R. Gilbertson UR - https://acs.figshare.com/articles/journal_contribution/Synthesis_and_Evaluation_of_Dimeric_Derivatives_of_5_HT_sub_2A_sub_Receptor_5_HT_sub_2A_sub_R_Antagonist_M_100907/2583343 DO - 10.1021/cn200077q.s001 L4 - https://ndownloader.figshare.com/files/4229308 KW - Dimeric Derivatives KW - HT KW - 2AR KW - dimeric version KW - 2A KW - oligmeric forms KW - antagonist KW - linker connection KW - serotonin receptors KW - receptor ligands KW - 18 atoms KW - linker length KW - polyether linkers N2 - It is now well accepted that at least some serotonin receptors exist in dimeric and oligmeric forms. The linking of receptor ligands has been shown to have potential in the development of selective agonists and antagonists for traditionally refractive receptors. Here we report the development of a dimeric version of the known 5-HT2AR antagonist, M-100907. Derivatives of M-100907 were synthesized to determine an appropriate site for the linker connection. Then, homodimers with polyether linkers of different lengths were functionally tested in a bioassay to determine the optimal linker length. Attachment at the catechol of M-100907 with linkers between 12 and 18 atoms in length proved to be optimal. ER -