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2. Design and Synthesis of New Transient Receptor Potential Vanilloid Type-1 (TRPV1) Channel Modulators: Identification, Molecular Modeling Analysis, and Pharmacological Characterization of the N-(4-Hydroxy-3-methoxybenzyl)-4-(thiophen-2-yl)butanamide, a Small Molecule Endowed with Agonist TRPV1 Activity and Protective Effects against Oxidative Stress

Author

Federico Corelli, Stefano Alcaro, Claudia Sticozzi, Vanessa Maestrini, Luciano De Petrocellis, Francesca Aiello, Francesca Guida, Antonella Brizzi, Marco Allarà, Mariateresa Badolato, Anna Artese, Livio Luongo, Vincenzo Di Marzo, Alessia Ligresti, Carlo Aldinucci, Giosuè Costa, Federica Pessina, Aniello Schiano Moriello, Giuseppe Valacchi, Maria Frosini, Sabatino Maione, Aiello, F, Badolato, M, Pessina, F, Sticozzi, C, Maestrini, V, Aldinucci, C, Luongo, Livio, Guida, Francesca, Ligresti, A, Artese, A, Allarà, M, Costa, G, Frosini, M, Schiano Moriello, A, De Petrocellis, L, Valacchi, G, Alcaro, S, Maione, Sabatino, Di Marzo, V, Corelli, F, and Brizzi, A.

Subjects
0301 basic medicine, Agonist, Male, Models, Molecular, antioxidant, Molecular model, Physiology, medicine.drug_class, Stereochemistry, antinociceptive, capsaicin, neuroprotective, oxidative stress, TRPV1 ligands, Biochemistry, Cell Biology, Cognitive Neuroscience, TRPV1, TRPV Cation Channels, CHO Cells, Thiophenes, NO, 03 medical and health sciences, chemistry.chemical_compound, Transient receptor potential channel, 0302 clinical medicine, Molecular recognition, Cricetulus, medicine, Animals, Rats, Wistar, Analgesics, Chemistry, General Medicine, Small molecule, Oxidative Stress, 030104 developmental biology, Capsaicin, Docking (molecular), 030217 neurology & neurosurgery
Abstract

4-(Thiophen-2-yl)butanoic acid was identified as a cyclic substitute of the unsaturated alkyl chain of the natural ligand, capsaicin. Accordingly, a new class of amides was synthesized in good yield and high purity and their molecular recognition against the target was investigated by means of docking experiments followed by molecular dynamics simulations, in order to rationalize their geometrical and thermodynamic profiles. The pharmacological properties of these new compounds were expressed as activation (EC50) and desensitization (IC50) potencies. Several compounds were found to activate TRPV1 channels, and in particular, derivatives 1 and 10 behaved as TRPV1 agonists endowed with good efficacy as compared to capsaicin. The most promising compound 1 was also evaluated for its protective role against oxidative stress on keratinocytes and differentiated human neuroblastoma cell lines expressing the TRPV1 receptor as well as for its cytotoxicity and analgesic activity in vivo.

Published
2016
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