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dc.contributor.author
Minguez Viñas, Teresa
dc.contributor.author
Nielsen, Beatriz Elizabeth
dc.contributor.author
Shoemark, Deborah K.
dc.contributor.author
Gotti, Cecilia
dc.contributor.author
Sessions, Richard B.
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Mulholland, Adrian J.
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Bouzat, Cecilia Beatriz
dc.contributor.author
Wonnacott, Susan
dc.contributor.author
Gallagher, Timothy
dc.contributor.author
Bermudez, Isabel
dc.contributor.author
Oliveira, Ana Sofia
dc.date.available
2021-06-29T13:27:57Z
dc.date.issued
2021-04
dc.identifier.citation
Minguez Viñas, Teresa; Nielsen, Beatriz Elizabeth; Shoemark, Deborah K.; Gotti, Cecilia; Sessions, Richard B.; et al.; A conserved arginine with non‐conserved function is a key determinant of agonist selectivity in α7 nicotinic ACh receptors; Wiley Blackwell Publishing, Inc; British Journal of Pharmacology; 178; 7; 4-2021; 1651-1668
dc.identifier.issn
0007-1188
dc.identifier.uri
http://hdl.handle.net/11336/135095
dc.description.abstract
The α7 and α4β2* (“*” denotes possibly assembly with another subunit) nicotinic acetylcholine receptors (nAChRs) are the most abundant nAChRs in the mammalian brain. These receptors are the most targeted nAChRs in drug discovery programmes for brain disorders. However, the development of subtype-specific agonists remains challenging due to the high degree of sequence homology and conservation of function in nAChRs. We have developed C(10) variants of cytisine, a partial agonist of α4β2 nAChR that has been used for smoking cessation. The C(10) methyl analogue used in this study displays negligible affinity for α7 nAChR, while retaining high affinity for α4β2 nAChR.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Wiley Blackwell Publishing, Inc
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights
Atribución-NoComercial-CompartirIgual 2.5 Argentina (CC BY-NC-SA 2.5 AR)
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
AGONIST SELECTIVITY
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C(10) CYSTINE DERIVATIVES
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CYSTINE
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NICOTINIC ACh 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
A conserved arginine with non‐conserved function is a key determinant of agonist selectivity in α7 nicotinic ACh receptors
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2021-06-10T19:28:14Z
dc.identifier.eissn
1476-5381
dc.journal.volume
178
dc.journal.number
7
dc.journal.pagination
1651-1668
dc.journal.pais
Estados Unidos
dc.journal.ciudad
New Jersey
dc.description.fil
Fil: Minguez Viñas, Teresa. Oxford Brookes University; Reino Unido
dc.description.fil
Fil: Nielsen, Beatriz Elizabeth. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
dc.description.fil
Fil: Shoemark, Deborah K.. University Of Bristol; Reino Unido
dc.description.fil
Fil: Gotti, Cecilia. Università degli Studi di Milano; Italia
dc.description.fil
Fil: Sessions, Richard B.. University Of Bristol; Reino Unido
dc.description.fil
Fil: Mulholland, Adrian J.. University Of Bristol; Reino Unido
dc.description.fil
Fil: Bouzat, Cecilia Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
dc.description.fil
Fil: Wonnacott, Susan. University of Bath; Reino Unido
dc.description.fil
Fil: Gallagher, Timothy. University Of Bristol; Reino Unido
dc.description.fil
Fil: Bermudez, Isabel. University of Oxford; Reino Unido
dc.description.fil
Fil: Oliveira, Ana Sofia. University Of Bristol; Reino Unido
dc.journal.title
British Journal of Pharmacology
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/10.1111/bph.15389
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1111/bph.15389
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