Structure-Activity Relationships of Phenylalkylamines as Agonist Ligands for 5-HT2AReceptors
| Autor: | Pieter Smid, Antoni R. Blaazer, Chris G. Kruse |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Agonist
medicine.drug_class Stereoisomerism Pharmacology Ligands Biochemistry Structure-Activity Relationship Drug Discovery medicine Animals Humans Structure–activity relationship Receptor Serotonin 5-HT2A Amines General Pharmacology Toxicology and Pharmaceutics Receptor Molecular Structure Human studies Chemistry Organic Chemistry Serotonin Receptor Agonists Drug Design Molecular Medicine Serotonin Signal transduction Serotonin 5-HT2 Receptor Agonists Endogenous agonist |
| Zdroj: | ChemMedChem. 3:1299-1309 |
| ISSN: | 1860-7187 1860-7179 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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