Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type 5 (mGlu5) receptor negative allosteric modula...

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Detalles Bibliográficos
Autores: Nonell, Santi, Bresolí-Obach, Roger, Font Inglès, Joan, López-Cano, Marc, Notartomaso, Serena, Scarselli, Pamela, Di Pietro, Paola, Battaglia, Giuseppe, Malhaire, Fanny, Rovira, Xavier, Catena, Juanlo, Giraldo, Jesús, Pin, Jean-Philippe, Fernández-Dueñas, Víctor, Goudet, Cyril, Nicoletti, Ferdinando, Llebaria, Amadeu, Ciruela, Francisco
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2017
País:España
Institución:Universitat Ramon Llull (URL)
Repositorio:DAU Arxiu Digital de la Universitat Ramon Llull
OAI Identifier:oai:dau.url.edu:20.500.14342/993
Acceso en línea:https://hdl.handle.net/20.500.14342/993
https://doi.org/10.7554/elife.23545
Access Level:acceso abierto
Palabra clave:Dolor--Tractament
Analgèsia
Malalties cròniques
Light-operated drugs
Complex diseases
Optical control
615
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spelling Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulatorNonell, SantiBresolí-Obach, RogerFont Inglès, JoanLópez-Cano, MarcNotartomaso, SerenaScarselli, PamelaDi Pietro, PaolaBattaglia, GiuseppeMalhaire, FannyRovira, XavierCatena, JuanloGiraldo, JesúsPin, Jean-PhilippeFernández-Dueñas, VíctorGoudet, CyrilNicoletti, FerdinandoLlebaria, AmadeuCiruela, FranciscoDolor--TractamentAnalgèsiaMalalties cròniquesLight-operated drugsComplex diseasesOptical control615Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type 5 (mGlu5) receptor negative allosteric modulator raseglurant. Violet light illumination of JF-NP-26 induces a photochemical reaction prompting the active-drug’s release, which effectively controls mGlu5 receptor activity both in ectopic expressing systems and in striatal primary neurons. Systemic administration in mice followed by local light-emitting diode (LED)-based illumination, either of the thalamus or the peripheral tissues, induced JF-NP-26-mediated light-dependent analgesia both in neuropathic and in acute/tonic inflammatory pain models. These data offer the first example of optical control of analgesia in vivo using a photocaged mGlu5 receptor negative allosteric modulator. This approach shows potential for precisely targeting, in time and space, endogenous receptors, which may allow a better management of difficult-to-treat disorders.eLife Sciences PublicationsUniversitat Ramon Llull. IQS20202023202020232017info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion20 p.application/pdfhttps://hdl.handle.net/20.500.14342/993https://doi.org/10.7554/elife.23545RECERCAT (Dipòsit de la Recerca de Catalunya)reponame:DAU Arxiu Digital de la Universitat Ramon Llullinstname:Universitat Ramon Llull (URL)IngléseLIFE. Vol.6 (2017), e23545info:eu-repo/grantAgreement/MINECO I ISCIII /PN I+D/SAF2014-55700-Pinfo:eu-repo/grantAgreement/MINECO I ISCIII /PN I+D/PCIN-2013–019 C03-03info:eu-repo/grantAgreement/MINECO I ISCIII/PN I+D/PIE14info:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-1054info:eu-repo/grantAgreement/ICREA/ICREA Academia-2010/info:eu-repo/grantAgreement/Fundació La Marató TV3/20152031/info:eu-repo/grantAgreement/IWT/SBO-140028/info:eu-repo/grantAgreement/MINECO/PN I+D/PCIN-2013–018 C03-02info:eu-repo/grantAgreement/MINECO/PN I+D/SAF2014-58396-Rinfo:eu-repo/grantAgreement/MINECO/PN I+D/PCIN-2013–017 C03-01info:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2014-57020-Rinfo:eu-repo/grantAgreement/SUR del DEC/2014CTP0002/info:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2013-48767-C3-1-Rinfo:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2015-71896-REDTinfo:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-109info:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-304info:eu-repo/grantAgreement/SUR del DEC i FSE/FI/2016 FI_B1 00021Attribution 4.0 International© L'autor/ahttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:dau.url.edu:20.500.14342/9932026-06-21T06:40:37Z
dc.title.none.fl_str_mv Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
title Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
spellingShingle Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
Nonell, Santi
Dolor--Tractament
Analgèsia
Malalties cròniques
Light-operated drugs
Complex diseases
Optical control
615
title_short Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
title_full Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
title_fullStr Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
title_full_unstemmed Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
title_sort Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
dc.creator.none.fl_str_mv Nonell, Santi
Bresolí-Obach, Roger
Font Inglès, Joan
López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández-Dueñas, Víctor
Goudet, Cyril
Nicoletti, Ferdinando
Llebaria, Amadeu
Ciruela, Francisco
author Nonell, Santi
author_facet Nonell, Santi
Bresolí-Obach, Roger
Font Inglès, Joan
López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández-Dueñas, Víctor
Goudet, Cyril
Nicoletti, Ferdinando
Llebaria, Amadeu
Ciruela, Francisco
author_role author
author2 Bresolí-Obach, Roger
Font Inglès, Joan
López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández-Dueñas, Víctor
Goudet, Cyril
Nicoletti, Ferdinando
Llebaria, Amadeu
Ciruela, Francisco
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universitat Ramon Llull. IQS
dc.subject.none.fl_str_mv Dolor--Tractament
Analgèsia
Malalties cròniques
Light-operated drugs
Complex diseases
Optical control
615
topic Dolor--Tractament
Analgèsia
Malalties cròniques
Light-operated drugs
Complex diseases
Optical control
615
description Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type 5 (mGlu5) receptor negative allosteric modulator raseglurant. Violet light illumination of JF-NP-26 induces a photochemical reaction prompting the active-drug’s release, which effectively controls mGlu5 receptor activity both in ectopic expressing systems and in striatal primary neurons. Systemic administration in mice followed by local light-emitting diode (LED)-based illumination, either of the thalamus or the peripheral tissues, induced JF-NP-26-mediated light-dependent analgesia both in neuropathic and in acute/tonic inflammatory pain models. These data offer the first example of optical control of analgesia in vivo using a photocaged mGlu5 receptor negative allosteric modulator. This approach shows potential for precisely targeting, in time and space, endogenous receptors, which may allow a better management of difficult-to-treat disorders.
publishDate 2017
dc.date.none.fl_str_mv 2017
2020
2020
2023
2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/20.500.14342/993
https://doi.org/10.7554/elife.23545
url https://hdl.handle.net/20.500.14342/993
https://doi.org/10.7554/elife.23545
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv eLIFE. Vol.6 (2017), e23545
info:eu-repo/grantAgreement/MINECO I ISCIII /PN I+D/SAF2014-55700-P
info:eu-repo/grantAgreement/MINECO I ISCIII /PN I+D/PCIN-2013–019 C03-03
info:eu-repo/grantAgreement/MINECO I ISCIII/PN I+D/PIE14
info:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-1054
info:eu-repo/grantAgreement/ICREA/ICREA Academia-2010/
info:eu-repo/grantAgreement/Fundació La Marató TV3/20152031/
info:eu-repo/grantAgreement/IWT/SBO-140028/
info:eu-repo/grantAgreement/MINECO/PN I+D/PCIN-2013–018 C03-02
info:eu-repo/grantAgreement/MINECO/PN I+D/SAF2014-58396-R
info:eu-repo/grantAgreement/MINECO/PN I+D/PCIN-2013–017 C03-01
info:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2014-57020-R
info:eu-repo/grantAgreement/SUR del DEC/2014CTP0002/
info:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2013-48767-C3-1-R
info:eu-repo/grantAgreement/MINECO/PN I+D/CTQ2015-71896-REDT
info:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-109
info:eu-repo/grantAgreement/SUR del DEC/SGR/2014-SGR-304
info:eu-repo/grantAgreement/SUR del DEC i FSE/FI/2016 FI_B1 00021
dc.rights.none.fl_str_mv Attribution 4.0 International
© L'autor/a
http://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution 4.0 International
© L'autor/a
http://creativecommons.org/licenses/by/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 20 p.
application/pdf
dc.publisher.none.fl_str_mv eLife Sciences Publications
publisher.none.fl_str_mv eLife Sciences Publications
dc.source.none.fl_str_mv RECERCAT (Dipòsit de la Recerca de Catalunya)
reponame:DAU Arxiu Digital de la Universitat Ramon Llull
instname:Universitat Ramon Llull (URL)
instname_str Universitat Ramon Llull (URL)
reponame_str DAU Arxiu Digital de la Universitat Ramon Llull
collection DAU Arxiu Digital de la Universitat Ramon Llull
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300719

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