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Development of an Indole-Amide-Based Photoswitchable Cannabinoid Receptor Subtype 1 (CB1R) “Cis-On” Agonist

dc.audienceTodo Públicospa
dc.citation.issue16
dc.citation.volume13
dc.contributor.advisorRamírez Rivera, Yesid Andres
dc.contributor.authorRamírez Rivera, Yesid Andres
dc.contributor.authorRodríguez Soacha, Diego A
dc.contributor.authorSteinmüller, Sophie AM
dc.contributor.authorIşbilir, Ali
dc.contributor.authorFender, Julia
dc.contributor.authorDeventer, Marie H
dc.contributor.authorTutov, Anna
dc.contributor.authorSotriffer, Christoph
dc.contributor.authorStove, Christophe P
dc.contributor.authorLorenz, Kristina
dc.contributor.authorLohse, Martín J
dc.contributor.authorHislop, James N
dc.contributor.authorDecker, Michael
dc.coverage.spatialWilliamsburg de Lat: 33 36 00 N degrees minutes Lat: 33.6000 decimal degrees Long: 087 03 00 W degrees minutes Long: -87.0500 decimal degreesspa
dc.date.accessioned2023-08-04T19:23:19Z
dc.date.available2023-08-04T19:23:19Z
dc.date.issued2022-07-26
dc.description.abstractActivation of the human cannabinoid receptor type 1 (hCB1R) with high spatiotemporal control is useful to study processes involved in different pathologies related to nociception, metabolic alterations, and neurological disorders. To synthesize new agonist ligands for hCB1R, we have designed different classes of photoswitchable molecules based on an indole core. The modifications made to the central core have allowed us to understand the molecular characteristics necessary to design an agonist with optimal pharmacological properties. Compound 27a shows high affinity for CB1R (Ki (cis-form) = 0.18 μM), with a marked difference in affinity with respect to its inactive “trans-off” form (CB1R Kitrans/cis ratio = 5.4). The novel compounds were evaluated by radioligand binding studies, receptor internalization, sensor receptor activation (GRABeCB2.0), Western blots for analysis of ERK1/2 activation, NanoBiT βarr2 recruitment, and calcium mobilization assays, respectively. The data show that the novel agonist 27a is a candidate for studying the optical modulation of cannabinoid receptors (CBRs), serving as a new molecular tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.spa
dc.format.extent25 páginasspa
dc.format.mediumDigitalspa
dc.format.mimetypehtlm
dc.identifier.doihttps://doi.org/10.1021/acschemneuro.2c00160
dc.identifier.instnameinstname:Universidad Icesispa
dc.identifier.reponamereponame:Biblioteca Digitalspa
dc.identifier.repourlrepourl:https://repository.icesi.edu.co/spa
dc.identifier.urihttp://hdl.handle.net/10906/104318
dc.language.isoengspa
dc.publisherAmerican Chemical Societyspa
dc.publisher.placeEstados Unidos Americaspa
dc.relation.citationendpage2435
dc.relation.citationstartpage2410
dc.relation.iscitedbyCS Chem. Neurosci. 2022 , 13 , 16 , 2410 - 2435
dc.relation.isreferencedbyPubMed: 35881914
dc.rights.accessrightsinfo:eu-repo/semantics/openAccessspa
dc.rights.coarhttp://purl.org/coar/access_right/c_abf2spa
dc.rights.licenseAtribución-NoComercial-SinDerivadas 4.0 Internacional (CC BY-NC-ND 4.0)
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subject.proposalAgonistsspa
dc.subject.proposalReceptorsspa
dc.subject.proposalLigandsspa
dc.subject.proposalAzobenzenespa
dc.subject.proposalG-protein-coupledspa
dc.subject.proposalreceptorspa
dc.subject.proposaldiazocinespa
dc.titleDevelopment of an Indole-Amide-Based Photoswitchable Cannabinoid Receptor Subtype 1 (CB1R) “Cis-On” Agonistspa
dc.type.coarhttp://purl.org/coar/resource_type/c_6501spa
dc.type.coarversionhttp://purl.org/coar/version/c_970fb48d4fbd8a85spa
dc.type.driverinfo:eu-repo/semantics/articlespa
dc.type.localArtículospa
dc.type.versioninfo:eu-repo/semantics/publishedVersionspa

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