Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2014 Jun 6

PMID 24900736

Citations 3

Authors

Claudio Battilocchio

Lucie Guetzoyan

Chiara Cervetto

Lorenzo Di Cesare Mannelli

Daniela Frattaroli

Ian R Baxendale

Guido Maura

Antonietta Rossi

Lidia Sautebin

Mariangela Biava

Carla Ghelardini

Manuela Marcoli

Steven V Ley

Affiliations

Soon will be listed here.

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.

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