Open AccessStructure–activity relationships of serotonin 5‐HT 2A agonists
Author(s) -
Nichols David E.
Publication year - 2012
Publication title -
wiley interdisciplinary reviews: membrane transport and signaling
Language(s) - English
Resource type - Journals
eISSN - 2190-4618
pISSN - 2190-460X
DOI - 10.1002/wmts.42
Subject(s) - hallucinogen , tryptamines , lysergic acid diethylamide , phenethylamines , 5 ht receptor , serotonin , 5 ht2a receptor , agonist , pharmacology , receptor , neuroscience , inverse agonist , lysergic acid , endogenous agonist , chemistry , psychology , biology , stereochemistry , biochemistry , tryptamine , dopamine receptor d1
Of the 14 known types of serotonin receptors one of the most extensively studied is the 5‐HT 2A (5‐hydroxytryptamine) receptor. In the brain, this receptor plays a key role in regulation of cortical function and cognition, appears to be the principal target for the hallucinogenic/psychedelic drugs such as lysergic acid diethylamide (LSD), and also is a target for the newest atypical antipsychotic agents, which are antagonists or inverse agonists at this site. Among the structure–activity relationships that are known for this receptor type, there are three chemical classes of agonists: tryptamines, ergolines, and phenethylamines. Important structural features are identified for agonist activity and some of these agonists have features in common. In addition to effects at the receptor will be the focus, these drugs are also hallucinogenic (psychedelic) agents, and much of the SAR was developed on the basis of effects in humans, before modern pharmacological techniques were available. A certain amount of our knowledge therefore relies on those human studies. WIREs Membr Transp Signal 2012, 1:559–579. doi: 10.1002/wmts.42 For further resources related to this article, please visit the WIREs website .