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 agonist...

Full description

Saved in:
Bibliographic Details
Published in:ChemMedChem 2008-09, Vol.3 (9), p.1299-1309
Main Authors: Blaazer, Antoni R, Smid, Pieter, Kruse, Chris G
Format: Article
Language:English
Subjects:
Amines - chemistry
Amines - pharmacology
Animals
Drug Design
Humans
Ligands
Molecular Structure
Receptor, Serotonin, 5-HT2A - genetics
Serotonin 5-HT2 Receptor Agonists
Serotonin Receptor Agonists - chemistry
Serotonin Receptor Agonists - pharmacology
Stereoisomerism
Structure-Activity Relationship
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1860-7187
DOI:10.1002/cmdc.200800133