Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT 2A Receptors

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...

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Published in:ChemMedChem 2008-09, Vol.3 (9), p.1299-1309
Main Authors: Blaazer, Antoni R., Smid, Pieter, Kruse, Chris G.
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description 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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title Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT 2A Receptors
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