High-potency ligands for DREADD imaging and activation in rodents and monkeys

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dc.contributor.authorBonaventura, Jordi
dc.contributor.authorEldridge, Mark A.G.
dc.contributor.authorHu, Feng
dc.contributor.authorGomez, Juan L.
dc.contributor.authorSánchez Soto, Marta
dc.contributor.authorAbramyan, Ara M.
dc.contributor.authorLam, Sherry
dc.contributor.authorBoehm, Matthew A.
dc.contributor.authorRuiz, Christina
dc.contributor.authorFarrell, Mitchell R.
dc.contributor.authorMoreno, Andrea
dc.contributor.authorGalal Faress, Islam Mustafa
dc.contributor.authorAndersen, Niels
dc.contributor.authorLinm John Y.
dc.contributor.authorMoaddel, Ruin
dc.contributor.authorMorris, Patrick J.
dc.contributor.authorShi, Lei
dc.contributor.authorSibley, David R.
dc.contributor.authorMahler, Stephen V.
dc.contributor.authorNabavi, Sadegh
dc.contributor.authorPomper, Martin G.
dc.contributor.authorBonci, Antonello
dc.contributor.authorHorti, Andrew G.
dc.contributor.authorRichmond, Barry J.
dc.contributor.authorMichaelides, Michael
dc.date.accessioned2022-11-08T18:56:24Z
dc.date.available2022-11-08T18:56:24Z
dc.date.issued2019-10-11
dc.date.updated2022-11-08T18:56:24Z
dc.description.abstractDesigner Receptors Exclusively Activated by Designer Drugs (DREADDs) are a popular chemogenetic technology for manipulation of neuronal activity in uninstrumented awake animals with potential for human applications as well. The prototypical DREADD agonist clozapine N-oxide (CNO) lacks brain entry and converts to clozapine, making it difficult to apply in basic and translational applications. Here we report the development of two novel DREADD agonists, JHU37152 and JHU37160, and the first dedicated 18F positron emission tomography (PET) DREADD radiotracer, [18F]JHU37107. We show that JHU37152 and JHU37160 exhibit high in vivo DREADD potency. [18F]JHU37107 combined with PET allows for DREADD detection in locally-targeted neurons, and at their long-range projections, enabling noninvasive and longitudinal neuronal projection mapping.
dc.format.extent12 p.
dc.format.mimetypeapplication/pdf
dc.identifier.idgrec712840
dc.identifier.issn2041-1723
dc.identifier.urihttps://hdl.handle.net/2445/190602
dc.language.isoeng
dc.publisherNature Publishing Group
dc.relation.isformatofReproducció del document publicat a: https://doi.org/10.1038/s41467-019-12236-z
dc.relation.ispartofNature Communications, 2019, vol. 10
dc.relation.projectIDinfo:eu-repo/grantAgreement/EC/H2020/679714/EU//STC
dc.relation.urihttps://doi.org/10.1038/s41467-019-12236-z
dc.rightscc-by (c) Bonaventura, Jordi et al., 2019
dc.rights.accessRightsinfo:eu-repo/semantics/openAccess
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.sourceArticles publicats en revistes (Patologia i Terapèutica Experimental)
dc.subject.classificationAnimals
dc.subject.classificationAntipsicòtics
dc.subject.classificationCervell
dc.subject.classificationDrogues de disseny
dc.subject.otherAnimals
dc.subject.otherAntipsychotic drugs
dc.subject.otherBrain
dc.subject.otherDesigner drugs
dc.titleHigh-potency ligands for DREADD imaging and activation in rodents and monkeys
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:eu-repo/semantics/publishedVersion

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Articles publicats en revistes (Patologia i Terapèutica Experimental)