{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Casey AB"],"funding":["National Institute of Neurological Disorders and Stroke","NIDA NIH HHS","U.S. Department of Defense","NINDS NIH HHS","National Institute on Drug Abuse","Northeastern University"],"pagination":["115028"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9252399"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["200"],"pubmed_abstract":["Blockade of the serotonin 5-HT<sub>2A</sub> G protein-coupled receptor (5-HT<sub>2A</sub>R) 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<sub>2A</sub>R by serotonergic psychedelics may be useful in treating neuropsychiatric indications, including major depressive and substance use disorders. Serotonergic psychedelics and other 5-HT<sub>2A</sub>R agonists, however, often bind other receptors, and standard 5-HT<sub>2A</sub>R antagonists lack sufficient selectivity to make well-founded mechanistic conclusions about the 5-HT<sub>2A</sub>R-dependent effects of these compounds and the general neurobio"],"journal":["Biochemical pharmacology"],"pubmed_title":["\"Selective\" serotonin 5-HT<sub>2A</sub> receptor antagonists."],"pmcid":["PMC9252399"],"funding_grant_id":["R01 DA030989","W81XWH-17-1-0329","R01DA047130","R01 DA047130","R15 NS118352","R01DA030989","R15 NS118352-01"],"pubmed_authors":["Cui M","Booth RG","Casey AB","Canal CE"],"additional_accession":[]},"is_claimable":false,"name":"\"Selective\" serotonin 5-HT<sub>2A</sub> receptor antagonists.","description":"Blockade of the serotonin 5-HT<sub>2A</sub> G protein-coupled receptor (5-HT<sub>2A</sub>R) 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<sub>2A</sub>R by serotonergic psychedelics may be useful in treating neuropsychiatric indications, including major depressive and substance use disorders. Serotonergic psychedelics and other 5-HT<sub>2A</sub>R agonists, however, often bind other receptors, and standard 5-HT<sub>2A</sub>R antagonists lack sufficient selectivity to make well-founded mechanistic conclusions about the 5-HT<sub>2A</sub>R-dependent effects of these compounds and the general neurobio","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Jun","modification":"2025-04-22T04:51:12.007Z","creation":"2025-04-05T21:08:49.028Z"},"accession":"S-EPMC9252399","cross_references":{"pubmed":["35381208"],"doi":["10.1016/j.bcp.2022.115028"]}}