biostudies-literatureBattilocchio CEngineering and Physical Sciences Research Council704-9https://www.ebi.ac.uk/biostudies/studies/S-EPMC4027228biostudies-literatureUnknown4(8)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.ACS medicinal chemistry lettersFlow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.PMC4027228EP/F069685/1Ghelardini CCervetto CBiava MDi Cesare Mannelli LBaxendale IRSautebin LBattilocchio CLey SVFrattaroli DMarcoli MMaura GRossi AGuetzoyan LfalseFlow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.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.2013-01-01T00:00:00Z2013 Aug2025-04-22T17:43:02.597Z2019-03-27T01:28:33ZS-EPMC40272282490073610.1021/ml400079h