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http://hdl.handle.net/10261/201363
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dc.contributor.author | Pérez de Vega, M. Jesús | - |
dc.contributor.author | Fernández-Mendívil, Cristina | - |
dc.contributor.author | Torre-Martínez, Roberto de la | - |
dc.contributor.author | González-Rodríguez, Sara | - |
dc.contributor.author | Mulet, José | - |
dc.contributor.author | Sala, Francisco | - |
dc.contributor.author | Sala, Salvador | - |
dc.contributor.author | Criado, Manuel | - |
dc.contributor.author | Moreno-Fernández, Silvia | - |
dc.contributor.author | Miguel, Marta | - |
dc.contributor.author | Fernández-Carvajal, Asia | - |
dc.contributor.author | Ferrer-Montiel, Antonio | - |
dc.contributor.author | López, Manuela G. | - |
dc.contributor.author | González-Muñiz, Rosario | - |
dc.date.accessioned | 2020-02-20T11:46:53Z | - |
dc.date.available | 2020-02-20T11:46:53Z | - |
dc.date.issued | 2019 | - |
dc.identifier | doi: 10.1021/acschemneuro.9b00364 | - |
dc.identifier | issn: 1948-7193 | - |
dc.identifier.citation | ACS Chemical Neuroscience 10: 3900-3909 (2019) | - |
dc.identifier.uri | http://hdl.handle.net/10261/201363 | - |
dc.description.abstract | Acetylcholine α7 nicotinic receptors are widely expressed in the brain, where they are involved in the central processing of pain as well as in neuropsychiatric, neurodegenerative, and inflammatory processes. Positive allosteric modulators (PAMs) show the advantage of allowing the selective regulation of different subtypes of acetylcholine receptors without directly interacting with the agonist binding site. Here, we report the preparation and biological activity of a fluoro-containing compound, 1-(2′,5′-dihydroxyphenyl)-3-(2-fluoro-4-hydroxyphenyl)-1-propanone (8, RGM079), that behaves as a potent PAM of the α7 receptors and has a balanced pharmacokinetic profile and antioxidant properties comparable or even higher than well-known natural polyphenols. In addition, compound RGM079 shows neuroprotective properties in Alzheimer's disease (AD)-toxicity related models. Thus, it causes a concentration-dependent neuroprotective effect against the toxicity induced by okadaic acid (OA) in the human neuroblastoma cell line SH-SY5Y. Similarly, in primary cultures of rat cortical neurons, RGM079 is able to restore the cellular viability after exposure to OA and amyloid peptide Aβ, with cell death almost completely prevented at 10 and 30 μM, respectively. Finally, compound RGM079 shows in vivo analgesic activity in the complete Freund's adjuvant (CFA)-induced paw inflammation model after intraperitoneal administration. | - |
dc.description.sponsorship | This work was supported by grants from the Spanish Ministerio de Economía y Competitividad (MINECO-FEDER) grant number SAF2015-66275-C2-R and RTI2018-097189-C2 to RGM and AFM, and RTI2018-095793-B-I00 to MGL, the Comunidad de Madrid/European Union Ref S2017/BMD-3827 to MGL and the CSIC, grant number 201980E030 to RGM. | - |
dc.language | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2015-66275-C2-R | - |
dc.relation | RTI2018-097189-C2/AEI/10.13039/501100011033 | - |
dc.relation | RTI2018-095793-B-I00/AEI/10.13039/501100011033 | - |
dc.relation | info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-097189-C2 | - |
dc.relation | info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-095793-B-I00 | - |
dc.relation | S2017/BMD-3827/NRF24AD-CM | - |
dc.relation.isversionof | Postprint | - |
dc.rights | openAccess | en_EN |
dc.subject | Diphenylpropanones | - |
dc.subject | α7 Nicotinic receptors | - |
dc.subject | Allosteric modulation | - |
dc.subject | Neuroprotection | - |
dc.subject | Analgesia | - |
dc.subject | Alzheimer disease | - |
dc.title | 1-(2′,5′-dihydroxyphenyl)-3-(2-fluoro-4-hydroxyphenyl)-1-propanone (RGM079): A positive allosteric modulator of α7 nicotinic receptors with analgesic and neuroprotective activity | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1021/acschemneuro.9b00364 | - |
dc.relation.publisherversion | http://dx.doi.org/10.1021/acschemneuro.9b00364 | - |
dc.embargo.terms | 2020-07-20 | - |
dc.date.updated | 2020-02-20T11:46:53Z | - |
dc.contributor.funder | Ministerio de Ciencia, Innovación y Universidades (España) | - |
dc.contributor.funder | Agencia Estatal de Investigación (España) | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.contributor.funder | European Commission | - |
dc.contributor.funder | Comunidad de Madrid | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100000780 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100011033 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/100012818 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
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ACS J Neurochem 2019. Pde Vega et al.pdf | 1,24 MB | Adobe PDF | Visualizar/Abrir |
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