{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Battilocchio C"],"funding":["Engineering and Physical Sciences Research Council"],"pagination":["704-9"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4027228"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["4(8)"],"pubmed_abstract":["We report the biological evaluation of a class of adamantane derivatives, which were achieved via modified telescoped machine-assisted flow procedure. Among the series of compounds tested in this work, 5 demonstrated outstanding analgesic properties. This compound showed that its action was not mediated through direct interaction with opioid and/or cannabinoid receptors. Moreover, it did not display any significant anti-inflammatory properties. Experiments carried out on rat cerebrocortical purified synaptosomes indicated that 5 inhibits the P2X7-evoked glutamate release, which may contribute to its antinociceptive properties. Nevertheless, further experiments are ongoing to characterize the pharmacological properties and mechanism of action of this molecule."],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release."],"pmcid":["PMC4027228"],"funding_grant_id":["EP/F069685/1"],"pubmed_authors":["Ghelardini C","Cervetto C","Biava M","Di Cesare Mannelli L","Baxendale IR","Sautebin L","Battilocchio C","Ley SV","Frattaroli D","Marcoli M","Maura G","Rossi A","Guetzoyan L"],"additional_accession":[]},"is_claimable":false,"name":"Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.","description":"We report the biological evaluation of a class of adamantane derivatives, which were achieved via modified telescoped machine-assisted flow procedure. Among the series of compounds tested in this work, 5 demonstrated outstanding analgesic properties. This compound showed that its action was not mediated through direct interaction with opioid and/or cannabinoid receptors. Moreover, it did not display any significant anti-inflammatory properties. Experiments carried out on rat cerebrocortical purified synaptosomes indicated that 5 inhibits the P2X7-evoked glutamate release, which may contribute to its antinociceptive properties. Nevertheless, further experiments are ongoing to characterize the pharmacological properties and mechanism of action of this molecule.","dates":{"release":"2013-01-01T00:00:00Z","publication":"2013 Aug","modification":"2025-04-22T17:43:02.597Z","creation":"2019-03-27T01:28:33Z"},"accession":"S-EPMC4027228","cross_references":{"pubmed":["24900736"],"doi":["10.1021/ml400079h"]}}