Structure–activity relationships of serotonin 5‐HT2Aagonists
Wiley Interdisciplinary Reviews Membrane Transport and Signalling February 28, 2012 David E. Nichols 80 citations
Of the 14 known serotonin receptor types, the 5-HT2A receptor is one of the most studied. In the brain, it regulates cortical function and cognition, is the main target for hallucinogenic drugs like LSD, and is also a target for newer atypical antipsychotic drugs that act as antagonists or inverse agonists. Three chemical classes of agonists exist: tryptamines, ergolines, and phenethylamines. Key structural features for agonist activity are identified, and some agonists share common features. Much of the structure-activity relationship knowledge comes from human studies conducted before modern pharmacological techniques.