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. KEYWORDS: Adamantane derivatives, 2-aminoadamantane-2-carboxylic acid, analgesic agents, flow chemistry, purinergic receptors
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7‐Evoked Glutamate Release / Battilocchio C; Guetzoyan L; Cervetto C; Di Cesare Mannelli L; Frattaroli D; Baxendale IR; Maura G; Rossi A; Sautebin L; Biava M; Ghelardini C; Marcoli M; Ley SV. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - STAMPA. - 4:(2013), pp. 704-709. [10.1021/ml400079h]
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7‐Evoked Glutamate Release
DI CESARE MANNELLI, LORENZO;GHELARDINI, CARLA;
2013
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. KEYWORDS: Adamantane derivatives, 2-aminoadamantane-2-carboxylic acid, analgesic agents, flow chemistry, purinergic receptorsFile | Dimensione | Formato | |
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Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7‐Evoked Glutamate Release.pdf
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