"Selective" serotonin 5-HT_2A receptor antagonists.

ABSTRACT: Blockade of the serotonin 5-HT_2A G protein-coupled receptor (5-HT_2AR) is a fundamental pharmacological characteristic of numerous antipsychotic medications, which are FDA-approved to treat schizophrenia, bipolar disorder, and as adjunctive therapies in major depressive disorder. Meanwhile, activation of the 5-HT_2AR by serotonergic psychedelics may be useful in treating neuropsychiatric indications, including major depressive and substance use disorders. Serotonergic psychedelics and other 5-HT_2AR agonists, however, often bind other receptors, and standard 5-HT_2AR antagonists lack sufficient selectivity to make well-founded mechanistic conclusions about the 5-HT_2AR-dependent effects of these compounds and the general neurobio

SUBMITTER: Casey AB 

PROVIDER: S-EPMC9252399 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature