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    Interaction of new sigma ligands with biomembrane models evaluated by differential scanning calorimetry and Langmuir-Blodgett studies

    Year: 2021

    Journal: Colloid Surf. B-Biointerfaces, Volume 201, MAY

    Authors: Marrazzo, Agostino; Torrisi, Cristina; Barbaraci, Carla; Amata, Emanuele; Castelli, Francesco; Sarpietro, Maria Grazia

    Keywords: Sigma 1; DMPC; Biomembrane model; MLV; Monolayer; DSC; Langmuir-Blodgett

    The compound (+)-MR200 [(+)-methyl (1R,2S)-2-{[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1phenylcyclopropanecarboxylate] is a selective sigma 1 (cs1) antagonist with antinociceptive effect, able to increase selective opioid receptor agonist-mediated analgesia. The parent compound (-)-MRV3 [(-)-methyl (1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)-methyl]-1-phenylcyclopropanecarboxylate], a cs1 antagonist with an improved cs1/cs2 selectivity respect to (+)-MR200, play a role in both central sensitization and pain hypersensitivity, suggesting a potential use of cs1 antagonists for the treatment of persistent pain conditions. With the intention to assessing the membrane absorption of compounds and their ability to cross it, the interaction of (+)-MR200 and (-)-MRV3 with dimyristoylphosphatidylcholine phospholipids (DMPC), used as biomembrane models was studied by Differential Scanning Calorimetry (DSC) and Langmuir-Blodgett (LB).
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