The synthesis of 5-HT2 receptor designed multiple ligands to investigate the role of the 5-HT2AR and the 5-HT2CR in cocaine addiction


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Previous studies indicate that the 5-HT2AR and 5-HT2CR play a role in cocaine induced behavior modification through either stimulation or inhibition respectively. Recent research has revealed that dimerization and oligomerization of GPCRs including the 5-HTRs frequently occurs. In order to target these GPCR dimers and oligomers bivalent ligands have been synthesized. Previously synthesized bivalent ligands have demonstrated increased affinity and potency when compared to administration of the monomers. The aim of this project is to synthesis homodimeric 5-HT2A R antagonists, homodimeric 5-HT2CR agonists, and heterodimeric 5-HT2A R antagonist/5-HT2CR agonist that will exhibit improved ability to control cocaine induced behavior modifications compared to the concurrent administration of a 5-HT2A R antagonist and a 5-HT2CR agonist.



designed multiple ligands, bivalent ligands, serotonin, 5-HT