The synthesis of WAY-derivatives to find linker location and a new linker to attach a fluorescence tag for homo- or hetero-dimer of 5-HT receptor ligands



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Serotonin action or inaction is known to correlate with depression, obesity and drug addiction. The serotonin receptor has been studied as a possible target for cocaine addiction therapy. Previously, 5-HT 2A receptor antagonist, M100907 and 5-HT 2C receptor agonist, WAY 163909 have been studied as molecules to control behaviors related to addiction. Additionally, serotonin receptor families such as 5-HT 2A and 5-H T2C receptors have been found to exist as dimers and oligomers. The focus of this thesis has been on the synthesis and bioactivity of multivalent ligands of M100907 and WAY 163909 for homo- and hetero dimeric ligands. As an extension of previous research, this study includes development of WAY derivatives, which can be developed for homo- or hetero dimeric ligands. In addition, a new linker for homodimers of M100907 derivatives has been developed. Through this new linker, a fluorescence tag can be attached to the dimeric ligands. This will be used to both probe the activity of receptor dimers as well as visualize them.



Multivalent ligands, 5-HT receptor