1374765-29-3Relevant articles and documents
Flow synthesis and biological studies of an analgesic adamantane derivative that inhibits P2X7-evoked glutamate release
Battilocchio, Claudio,Guetzoyan, Lucie,Cervetto, Chiara,Di Cesare Mannelli, Lorenzo,Frattaroli, Daniela,Baxendale, Ian R.,Maura, Guido,Rossi, Antonietta,Sautebin, Lidia,Biava, Mariangela,Ghelardini, Carla,Marcoli, Manuela,Ley, Steven V.
supporting information, p. 704 - 709 (2013/09/02)
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.