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Title

1,3-diphenylpropan-1-ones as allosteric modulators of α7 nACh receptors with analgesic and antioxidant properties

AuthorsCriado, Manuel; Balsera, Beatriz; Mulet Soler, José; Sala, Salvador; Torre-Martínez, Roberto de la; Fernández-Carvajal, Asia; Ferrer-Montiel, Antonio; Moreno-Fernández, Silvia; Miguel, Marta ; Pérez de Vega, M. Jesús; González-Muñiz, Rosario
KeywordsAlpha7 nAChR
Pain
Inflammation
Antioxidant
Positive allosteric modulator
Issue Date2016
PublisherFuture Science
CitationFuture Medicinal Chemistry 8: 731-749 (2016)
AbstractNicotine acethylcholine receptors (nAChRs) play critical roles in cognitive processes, neuroprotection and inflammation. Results: According to their substituents, 1,3-diphenylpropan-1-one derivatives act as α7 nAChRs negative allosteric modulators (NAM, OMe) or Type I positive allosteric modulators (PAMs, OH). Compounds 7 and 31 were the most effective (989 and 666% enhancement of ACh-induced currents) and potent (EC: 12.9 and 6.85 μM) PAMs. They exhibited strong radical scavenging values. Compound 31, selective over other neuronal nAChR subtypes and with acceptable pharmacokinetic profile, showed antinociceptive effects in a model of inflammatory pain. Conclusion: Compound 31 is a novel, potent and selective α7 nAChR PAM, displaying antioxidant and analgesic activities. The 1,3-diphenylpropan-1-one scaffold could be the base toward more advanced type I PAMs for the treatment of nAChR-mediated diseases.
Publisher version (URL)http://dx.doi.org/10.4155/fmc-2015-0001
URIhttp://hdl.handle.net/10261/141535
DOI10.4155/fmc-2015-0001
Identifiersdoi: 10.4155/fmc-2015-0001
issn: 1756-8919
e-issn: 1756-8927
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