{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Chen Y"],"funding":["NIDA NIH HHS","College of Pharmacy, Mercer University","National Institute on Drug Abuse"],"pagination":["960-968"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7104417"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["11(6)"],"pubmed_abstract":["Synthetic cathinones (SCs) are designer, psychostimulant drugs of abuse that primarily act on monoamine transporters; little is known about their off-target liability. Abuse of pyrrolidine-containing SCs, such as α-PHP, has been linked to clinical features, including tachycardia and hypertension, and psychiatric events, including delusions and memory impairments-effects mimicking deliriant hallucinogens that are acetylcholine muscarinic receptor (MR) antagonists. α-PHP and nine analogs with modifications in the α-carbon side chain length and/or containing a methylenedioxy moiety were screened for activity at each of the five human MRs. Increasing the length of the α-carbon side chain of 1-phenyl-2-(pyrrolidin-1-yl)ethan-1-one analogs from a methyl (α-PPP) to a propyl (α-PVP) group caused a"],"journal":["ACS chemical neuroscience"],"pubmed_title":["Structure-Activity Relationship Study of Psychostimulant Synthetic Cathinones Reveals Nanomolar Antagonist Potency of α-Pyrrolidinohexiophenone at Human Muscarinic M<sub>2</sub> Receptors."],"pmcid":["PMC7104417"],"funding_grant_id":["R21DA040907","R21 DA040907"],"pubmed_authors":["Chen Y","Canal CE"],"additional_accession":[]},"is_claimable":false,"name":"Structure-Activity Relationship Study of Psychostimulant Synthetic Cathinones Reveals Nanomolar Antagonist Potency of α-Pyrrolidinohexiophenone at Human Muscarinic M<sub>2</sub> Receptors.","description":"Synthetic cathinones (SCs) are designer, psychostimulant drugs of abuse that primarily act on monoamine transporters; little is known about their off-target liability. Abuse of pyrrolidine-containing SCs, such as α-PHP, has been linked to clinical features, including tachycardia and hypertension, and psychiatric events, including delusions and memory impairments-effects mimicking deliriant hallucinogens that are acetylcholine muscarinic receptor (MR) antagonists. α-PHP and nine analogs with modifications in the α-carbon side chain length and/or containing a methylenedioxy moiety were screened for activity at each of the five human MRs. Increasing the length of the α-carbon side chain of 1-phenyl-2-(pyrrolidin-1-yl)ethan-1-one analogs from a methyl (α-PPP) to a propyl (α-PVP) group caused a","dates":{"release":"2020-01-01T00:00:00Z","publication":"2020 Mar","modification":"2025-04-18T16:41:27.191Z","creation":"2025-04-07T04:05:10.7Z"},"accession":"S-EPMC7104417","cross_references":{"pubmed":["32073252"],"doi":["10.1021/acschemneuro.0c00008"]}}