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dc.contributor.author
Arias, Hugo R.
dc.contributor.author
Ghelardini, Carla
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Lucarini, Elena
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Tae, Han Shen
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Yousuf, Arsalan
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Marcovich, Irina
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Manetti, Dina
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Romanelli, Maria Novella
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Elgoyhen, Ana Belen
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Adams, David J.
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Di Cesare Mannelli, Lorenzo
dc.date.available
2021-03-19T18:54:50Z
dc.date.issued
2020-10-19
dc.identifier.citation
Arias, Hugo R.; Ghelardini, Carla; Lucarini, Elena; Tae, Han Shen; Yousuf, Arsalan; et al.; (E)-3-Furan-2-yl- N- p-tolyl-acrylamide and its Derivative DM489 Decrease Neuropathic Pain in Mice Predominantly by α7 Nicotinic Acetylcholine Receptor Potentiation; American Chemical Society; ACS Chemical Neuroscience; 11; 21; 19-10-2020; 3603-3614
dc.identifier.issn
1948-7193
dc.identifier.uri
http://hdl.handle.net/11336/128689
dc.description.abstract
The main objective of this study was to determine whether (E)-3-furan-2-yl-N-p-tolyl-acrylamide (PAM-2) and its structural derivative DM489 produce anti-neuropathic pain activity using the streptozotocin (STZ)- and oxaliplatin-induced neuropathic pain animal models. To assess possible mechanisms of action, the pharmacological activity of these compounds was determined at α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) and CaV2.2 channels expressed alone or coexpressed with G protein-coupled GABAB receptors. The animal results indicated that a single dose of 3 mg/kg PAM-2 or DM489 decreases STZ-induced neuropathic pain in mice, and chemotherapy-induced neuropathic pain is decreased by PAM-2 (3 mg/kg) and DM489 (10 mg/kg). The observed anti-neuropathic pain activity was inhibited by the α7-selective antagonist methyllycaconitine. The coadministration of oxaliplatin with an inactive dose (1 mg/kg) of PAM-2 decreased the development of neuropathic pain after 14, but not 7, days of cotreatment. The electrophysiological results indicated that PAM-2 potentiates human (h) and rat (r) α7 nAChRs with 2-7 times higher potency than that for hCaV2.2 channel inhibition and an even greater difference compared to that for rα9α10 nAChR inhibition. These results support the notion that α7 nAChR potentiation is likely the predominant molecular mechanism underlying the observed anti-nociceptive pain activity of these compounds.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
American Chemical Society
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
CAV2.2 CHANNELS
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NEUROPATHIC PAIN
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NICOTINIC ACETYLCHOLINE RECEPTORS
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POSITIVE ALLOSTERIC MODULATORS
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Neurociencias
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Medicina Básica
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CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
(E)-3-Furan-2-yl- N- p-tolyl-acrylamide and its Derivative DM489 Decrease Neuropathic Pain in Mice Predominantly by α7 Nicotinic Acetylcholine Receptor Potentiation
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2021-03-15T14:32:38Z
dc.journal.volume
11
dc.journal.number
21
dc.journal.pagination
3603-3614
dc.journal.pais
Estados Unidos
dc.description.fil
Fil: Arias, Hugo R.. Oklahoma State University; Estados Unidos
dc.description.fil
Fil: Ghelardini, Carla. Università degli Studi di Firenze; Italia
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Fil: Lucarini, Elena. Università degli Studi di Firenze; Italia
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Fil: Tae, Han Shen. University Of Wollongong; Australia
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Fil: Yousuf, Arsalan. University Of Wollongong; Australia
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Fil: Marcovich, Irina. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Investigación en Ingeniería Genética y Biología Molecular "Dr. Héctor N. Torres". Grupo Vinculado al INGEBI- Laboratorio de Biocatálisis y Biotransformaciones - LBB - UNQUI; Argentina
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Fil: Manetti, Dina. Università degli Studi di Firenze; Italia
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Fil: Romanelli, Maria Novella. Università degli Studi di Firenze; Italia
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Fil: Elgoyhen, Ana Belen. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Investigación en Ingeniería Genética y Biología Molecular "Dr. Héctor N. Torres". Grupo Vinculado al INGEBI- Laboratorio de Biocatálisis y Biotransformaciones - LBB - UNQUI; Argentina. Universidad de Buenos Aires; Argentina
dc.description.fil
Fil: Adams, David J.. University Of Wollongong; Australia
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Fil: Di Cesare Mannelli, Lorenzo. Università degli Studi di Firenze; Italia
dc.journal.title
ACS Chemical Neuroscience
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/acschemneuro.0c00476
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/acschemneuro.0c00476
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