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dc.contributor.author
Bagdas, Deniz
dc.contributor.author
Sevdar, Gulce
dc.contributor.author
Gul, Zulfiye
dc.contributor.author
Younis, Rabha
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Cavun, Sinan
dc.contributor.author
Tae, Han Shen
dc.contributor.author
Ortells, Marcelo Oscar
dc.contributor.author
Arias, Hugo R.
dc.contributor.author
Gurun, Mine Sibel
dc.date.available
2022-02-04T14:57:15Z
dc.date.issued
2021-07-19
dc.identifier.citation
Bagdas, Deniz; Sevdar, Gulce; Gul, Zulfiye; Younis, Rabha; Cavun, Sinan; et al.; (E)-3-furan-2-yl-N-phenylacrylamide (PAM-4) decreases nociception and emotional manifestations of neuropathic pain in mice by α7 nicotinic acetylcholine receptor potentiation; Maney Publishing; Neurological Research; 43; 12; 19-7-2021; 1056-1068
dc.identifier.issn
0161-6412
dc.identifier.uri
http://hdl.handle.net/11336/151352
dc.description.abstract
Clinical intervention of pain is often accompanied by changes in affective behaviors, so both assays of affective and sensorial aspects of nociception play an important role in the development of novel analgesics. Although positive allosteric modulation (PAM) of α7 nicotinic acetylcholine receptors (nAChRs) has been recognized as a novel approach for the relief of sensorial aspects of pain, their effects on affective components of pain remain unclear. Therefore, we investigated whether PAM-4, a highly selective α7-nAChR PAM, attenuates inflammatory and neuropathic pain, as well as the concomitant depressive/anxiety comorbidities. The anti-nociceptive activity of PAM-4 was assessed in mice using the formalin test and chronic constriction injury (CCI)-induced neuropathic pain model. The anxiolytic- and antidepressant-like activity of PAM-4 was evaluated using the marble burying test and forced swimming test. Acute systemic administration of PAM-4 dose-dependently reversed formalin-induced paw licking behavior and CCI-induced mechanical allodynia without development of any motor impairment. PAM-4 reversed the decreased swimming time and number of buried marbles in CCI-treated mice, suggesting that this ligand attenuates chronic pain-induced depression-like behavior and anxiogenic-like effects. The effects of PAM-4 were inhibited by the α7-selective antagonist methyllycaconitine, indicating molecular mechanism mediated by α7-nAChRs. Indeed, electrophysiological recordings showed the PAM-4 enhances human α7 nAChRs with higher potency and efficacy compared to rat α7 nAChRs. These findings suggest that PAM-4 reduces both sensorial and affective behaviors induced by chronic pain in mice by α7-nAChR potentiation. PAM-4 deserves further investigations for the management of chronic painful conditions with comorbidities.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Maney Publishing
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
CHRONIC CONSTRICTION INJURY
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ELECTROPHYSIOLOGY
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FORMALIN
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NEUROPATHIC PAIN
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PAM-4
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POSITIVE ALLOSTERIC MODULATOR
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Α7 NICOTINIC ACETYLCHOLINE RECEPTORS
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Bioquímica y Biología Molecular
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Ciencias Biológicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
(E)-3-furan-2-yl-N-phenylacrylamide (PAM-4) decreases nociception and emotional manifestations of neuropathic pain in mice 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
2022-01-25T15:01:23Z
dc.identifier.eissn
1743-1328
dc.journal.volume
43
dc.journal.number
12
dc.journal.pagination
1056-1068
dc.journal.pais
Reino Unido
dc.journal.ciudad
Londres
dc.description.fil
Fil: Bagdas, Deniz. University of Yale. School of Medicine; Estados Unidos
dc.description.fil
Fil: Sevdar, Gulce. Bursa Uludag University; Turquía
dc.description.fil
Fil: Gul, Zulfiye. Bahcesehir University; Turquía
dc.description.fil
Fil: Younis, Rabha. Virginia Commonwealth University; Estados Unidos
dc.description.fil
Fil: Cavun, Sinan. Bursa Uludag University; Turquía
dc.description.fil
Fil: Tae, Han Shen. University of Wollongong; Australia
dc.description.fil
Fil: Ortells, Marcelo Oscar. Universidad de Morón. Facultad de Medicina; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Arias, Hugo R.. Oklahoma State University; Estados Unidos
dc.description.fil
Fil: Gurun, Mine Sibel. Bursa Uludag University; Turquía
dc.journal.title
Neurological Research
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/full/10.1080/01616412.2021.1949684
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1080/01616412.2021.1949684
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