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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Autores: Font, Joan, López-Cano, Marc, Notartomaso, Serena, Scarselli, Pamela, Di Pietro, Paola, Bresolí-Obach, Roger, Battaglia, Giuseppe, Malhaire, Fanny, Rovira, Xavier, Catena, Juanlo, Giraldo, Jesús, Pin, Jean-Philippe, Fernández Dueñas, Víctor, Goudet, Cyril, Nonell, Santi, Nicoletti, Ferdinando, Llebaria Soldevila, Amadeu, Ciruela Alférez, Francisco
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2017
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/122570
Acceso en línea:https://hdl.handle.net/2445/122570
Access Level:acceso abierto
Palabra clave:Neurociències
Ratolins (Animals de laboratori)
Farmacologia
Tractament del dolor
Neurosciences
Mice (Laboratory animals)
Pharmacology
Pain treatment
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repository_id_str
spelling Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulatorFont, JoanLópez-Cano, MarcNotartomaso, SerenaScarselli, PamelaDi Pietro, PaolaBresolí-Obach, RogerBattaglia, GiuseppeMalhaire, FannyRovira, XavierCatena, JuanloGiraldo, JesúsPin, Jean-PhilippeFernández Dueñas, VíctorGoudet, CyrilNonell, SantiNicoletti, FerdinandoLlebaria Soldevila, AmadeuCiruela Alférez, FranciscoNeurociènciesRatolins (Animals de laboratori)FarmacologiaTractament del dolorNeurosciencesMice (Laboratory animals)PharmacologyPain treatmentLight-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 Sciences2018201820172018info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion20 p.application/pdfhttps://hdl.handle.net/2445/122570Articles publicats en revistes (Patologia i Terapèutica Experimental)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésReproducció del document publicat a: https://doi.org/10.7554/eLife.23545eLife, 2017, vol. 6, p. e23545https://doi.org/10.7554/eLife.23545cc-by (c) Font, Joan et al., 2017http://creativecommons.org/licenses/by/3.0/esinfo:eu-repo/semantics/openAccessoai:recercat.cat:2445/1225702026-05-29T05:05:01Z
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
Font, Joan
Neurociències
Ratolins (Animals de laboratori)
Farmacologia
Tractament del dolor
Neurosciences
Mice (Laboratory animals)
Pharmacology
Pain treatment
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 Font, Joan
López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Bresolí-Obach, Roger
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández Dueñas, Víctor
Goudet, Cyril
Nonell, Santi
Nicoletti, Ferdinando
Llebaria Soldevila, Amadeu
Ciruela Alférez, Francisco
author Font, Joan
author_facet Font, Joan
López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Bresolí-Obach, Roger
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández Dueñas, Víctor
Goudet, Cyril
Nonell, Santi
Nicoletti, Ferdinando
Llebaria Soldevila, Amadeu
Ciruela Alférez, Francisco
author_role author
author2 López-Cano, Marc
Notartomaso, Serena
Scarselli, Pamela
Di Pietro, Paola
Bresolí-Obach, Roger
Battaglia, Giuseppe
Malhaire, Fanny
Rovira, Xavier
Catena, Juanlo
Giraldo, Jesús
Pin, Jean-Philippe
Fernández Dueñas, Víctor
Goudet, Cyril
Nonell, Santi
Nicoletti, Ferdinando
Llebaria Soldevila, Amadeu
Ciruela Alférez, Francisco
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Neurociències
Ratolins (Animals de laboratori)
Farmacologia
Tractament del dolor
Neurosciences
Mice (Laboratory animals)
Pharmacology
Pain treatment
topic Neurociències
Ratolins (Animals de laboratori)
Farmacologia
Tractament del dolor
Neurosciences
Mice (Laboratory animals)
Pharmacology
Pain treatment
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
2018
2018
2018
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/2445/122570
url https://hdl.handle.net/2445/122570
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.7554/eLife.23545
eLife, 2017, vol. 6, p. e23545
https://doi.org/10.7554/eLife.23545
dc.rights.none.fl_str_mv cc-by (c) Font, Joan et al., 2017
http://creativecommons.org/licenses/by/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Font, Joan et al., 2017
http://creativecommons.org/licenses/by/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 20 p.
application/pdf
dc.publisher.none.fl_str_mv eLife Sciences
publisher.none.fl_str_mv eLife Sciences
dc.source.none.fl_str_mv Articles publicats en revistes (Patologia i Terapèutica Experimental)
reponame:Recercat. Dipósit de la Recerca de Catalunya
instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
instname_str Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
reponame_str Recercat. Dipósit de la Recerca de Catalunya
collection Recercat. Dipósit de la Recerca de Catalunya
repository.name.fl_str_mv
repository.mail.fl_str_mv
_version_ 1869423888191979520
score 15,811543

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