{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Alhosan N"],"funding":["Medical Research Council"],"pagination":["969-987"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7618119"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["182(4)"],"pubmed_abstract":["<h4>Background and purpose</h4>Fentanyls and nitazenes are μ-opioid receptor agonists responsible for a large number of opioid overdose deaths. Here, we determined the potency, dissociation kinetics and antagonism by naloxone at the μ receptor of several fentanyl and nitazene analogues, compared to morphine and DAMGO.<h4>Experimental approach</h4>In vitro assays of G protein activation and signalling and arrestin recruitment were performed. AtT20 cells expressing μ receptors were loaded with a membrane potential dye and changes in fluorescence used to determine agonist potency, dissociation kinetics and susceptibility to antagonism by naloxone. BRET experiments were undertaken in HEK293T cells expressing μ receptors to assess Gi protein activation and β-arrestin 2 recruitment.<h4>Key resul"],"journal":["British journal of pharmacology"],"pubmed_title":["Slow dissociation kinetics of fentanyls and nitazenes correlates with reduced sensitivity to naloxone reversal at the μ-opioid receptor."],"pmcid":["PMC7618119"],"funding_grant_id":["MR/ S010890/1","MR/S010890/1"],"pubmed_authors":["Kelly E","Henderson G","Santiago M","Alhosan N","Cavallo D"],"additional_accession":[]},"is_claimable":false,"name":"Slow dissociation kinetics of fentanyls and nitazenes correlates with reduced sensitivity to naloxone reversal at the μ-opioid receptor.","description":"<h4>Background and purpose</h4>Fentanyls and nitazenes are μ-opioid receptor agonists responsible for a large number of opioid overdose deaths. Here, we determined the potency, dissociation kinetics and antagonism by naloxone at the μ receptor of several fentanyl and nitazene analogues, compared to morphine and DAMGO.<h4>Experimental approach</h4>In vitro assays of G protein activation and signalling and arrestin recruitment were performed. AtT20 cells expressing μ receptors were loaded with a membrane potential dye and changes in fluorescence used to determine agonist potency, dissociation kinetics and susceptibility to antagonism by naloxone. BRET experiments were undertaken in HEK293T cells expressing μ receptors to assess Gi protein activation and β-arrestin 2 recruitment.<h4>Key resul","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Feb","modification":"2026-06-01T06:32:38.357Z","creation":"2026-04-08T10:02:43.716Z"},"accession":"S-EPMC7618119","cross_references":{"pubmed":["39437833"],"doi":["10.1111/bph.17376"]}}