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ChemMedChem. 2008 Sep;3(9):1299-309. doi: 10.1002/cmdc.200800133.

Structure-activity relationships of phenylalkylamines as agonist ligands for 5-HT(2A) receptors.

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  • 1Swammerdam Institute for Life Sciences, Centre for NeuroScience, University of Amsterdam, Kruislaan 320, 1098 SM Amsterdam.


Agonist activation of central 5-HT(2A) receptors results in diverse effects, such as hallucinations and changes of consciousness. Recent findings indicate that activation of the 5-HT(2A) receptor also leads to interesting physiological responses, possibly holding therapeutic value. Selective agonists are needed to study the full therapeutic potential of this receptor. 5-HT(2A) ligands with agonist profiles are primarily derived from phenylalkylamines, indolealkylamines, and certain piperazines. Of these, phenylalkylamines, most notably substituted phenylisopropylamines, are considered the most selective agonists for 5-HT(2) receptors. This review summarizes the structure-activity relationships (SAR) of phenylalkylamines as agonist ligands for 5-HT(2A) receptors. Selectivity is a central theme, as is selectivity for the 5-HT(2A) receptor and for its specific signaling pathways. SAR data from receptor affinity studies, functional assays, behavioral drug discrimination as well as human studies are discussed.

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