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dc.contributor.author
Arias, Hugo Rubén
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dc.contributor.author
Jin, Xiao Tao
dc.contributor.author
Gallino, Sofia Ludmila
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dc.contributor.author
Peng, Can
dc.contributor.author
Feuerbach, Dominik
dc.contributor.author
García Colunga, Jesús
dc.contributor.author
Elgoyhen, Ana Belen
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dc.contributor.author
Drenan, Ryan M.
dc.contributor.author
Ortells, Marcelo Oscar
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dc.date.available
2020-12-17T20:07:07Z
dc.date.issued
2019-12
dc.identifier.citation
Arias, Hugo Rubén; Jin, Xiao Tao; Gallino, Sofia Ludmila; Peng, Can; Feuerbach, Dominik; et al.; Selectivity of (±)-citalopram at nicotinic acetylcholine receptors and different inhibitory mechanisms between habenular α3β4* and α9α10 subtypes; Pergamon-Elsevier Science Ltd; Neurochemistry International; 131; 104552; 12-2019; 1-14
dc.identifier.issn
0197-0186
dc.identifier.uri
http://hdl.handle.net/11336/120790
dc.description.abstract
The inhibitory activity of (±)-citalopram on human (h) α3β4, α4β2, and α7 nicotinic acetylcholine receptors(AChRs) was determined by Ca2+ influx assays, whereas its effect on rat α9α10 and mouse habenular α3β4*AChRs by electrophysiological recordings. The Ca2+ influx results clearly establish that (±)-citalopram inhibits(IC50´s in μM) hα3β4 AChRs (5.1 ± 1.3) with higher potency than that for hα7 (18.8 ± 1.1) and hα4β2(19.1 ± 4.2) AChRs. This is in agreement with the [3H]imipramine competition binding results indicating that(±)-citalopram binds to imipramine sites at desensitized hα3β4 with>2-fold higher affinity than that forhα4β2. The electrophysiological, molecular docking, and in silico mutation results indicate that (±)-citalopramcompetitively inhibits rα9α10 AChRs (7.5 ± 0.9) in a voltage-independent manner by interacting mainly withorthosteric sites, whereas it inhibits a homogeneous population of α3β4* AChRs at MHb (VI) neurons(7.6 ± 1.0) in a voltage-dependent manner by interacting mainly with a luminal site located in the middle ofthe ion channel, overlapping the imipramine site, which suggests an ion channel blocking mechanism. In conclusion,(±)-citalopram inhibits α3β4 and α9α10 AChRs with higher potency compared to other AChRs but bydifferent mechanisms. (±)-Citalopram also inhibits habenular α3β4*AChRs, supporting the notion that thesereceptors are important endogenous targets related to their anti-addictive activities.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Pergamon-Elsevier Science Ltd
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
(±)-CITALOPRAM
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BRAIN SLICES
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MEDIAL HABENULA
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NICOTINIC ACETYLCHOLINE RECEPTOR
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SELECTIVE SEROTONIN REUPTAKE INHIBITOR
dc.subject.classification
Farmacología y Farmacia
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dc.subject.classification
Medicina Básica
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dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
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dc.title
Selectivity of (±)-citalopram at nicotinic acetylcholine receptors and different inhibitory mechanisms between habenular α3β4* and α9α10 subtypes
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-11-18T21:17:32Z
dc.journal.volume
131
dc.journal.number
104552
dc.journal.pagination
1-14
dc.journal.pais
Estados Unidos
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dc.description.fil
Fil: Arias, Hugo Rubén. Oklahoma State University; Estados Unidos
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Fil: Jin, Xiao Tao. Northwestern University; Estados Unidos
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Fil: Gallino, Sofia Ludmila. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Investigaciones en Ingeniería Genética y Biología Molecular "Dr. Héctor N. Torres"; Argentina
dc.description.fil
Fil: Peng, Can. Northwestern University; Estados Unidos
dc.description.fil
Fil: Feuerbach, Dominik. Novartis Institutes for Biomedical Research; Suiza
dc.description.fil
Fil: García Colunga, Jesús. Universidad Nacional Autónoma de México; México
dc.description.fil
Fil: Elgoyhen, Ana Belen. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Investigaciones en Ingeniería Genética y Biología Molecular "Dr. Héctor N. Torres"; Argentina. Universidad de Buenos Aires. Facultad de Medicina. Instituto de Farmacologia; Argentina
dc.description.fil
Fil: Drenan, Ryan M.. Northwestern University; Estados Unidos
dc.description.fil
Fil: Ortells, Marcelo Oscar. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Morón; Argentina
dc.journal.title
Neurochemistry International
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://linkinghub.elsevier.com/retrieve/pii/S0197018619303651
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.neuint.2019.104552
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