Pharmacological insights emerging from the characterization of a large collection of synthetic cannabinoid receptor agonists designer drugs

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dc.contributor.authorGioe-Gallo, Claudia
dc.contributor.authorOrtigueira, Sandra
dc.contributor.authorBrea, Jose
dc.contributor.authorRaich, Iu
dc.contributor.authorAzuaje, Jhonny
dc.contributor.authorPaleo, M. Rita
dc.contributor.authorMajellaro, Maria
dc.contributor.authorLoza, Maria Isabel
dc.contributor.authorSalas, Cristian O.
dc.contributor.authorGarcia-Mera, Xerardo
dc.contributor.authorNavarro, Gemma
dc.contributor.authorSotelo, Eddy
dc.date.accessioned2025-01-20T20:10:19Z
dc.date.available2025-01-20T20:10:19Z
dc.date.issued2023
dc.description.abstractSynthetic cannabinoid receptor agonists (SCRAs) constitute the largest and most defiant group of abuse designer drugs. These new psychoactive substances (NPS), developed as unregulated alternatives to cannabis, have potent cannabimimetic effects and their use is usually associated with episodes of psychosis, seizures, dependence, organ toxicity and death. Due to their ever-changing structure, very limited or nil structural, pharmacological, and toxicological information is available to the scientific community and the law enforcement offices. Here we report the synthesis and pharmacological evaluation (binding and functional) of the largest and most diverse collection of enantiopure SCRAs published to date. Our results revealed novel SCRAs that could be (or may currently be) used as illegal psychoactive substances. We also report, for the first time, the cannabimimetic data of 32 novel SCRAs containing an (R) configuration at the stereogenic center. The systematic pharmacological profiling of the library enabled the identification of emerging Structure-Activity Relationship (SAR) and Structure-Selectivity Relationship (SSR) trends, the detection of ligands exhibiting incipient cannabinoid re-ceptor type 2 (CB2R) subtype selectivity and highlights the significant neurotoxicity of representative SCRAs on mouse primary neuronal cells. Several of the new emerging SCRAs are currently expected to have a rather limited potential for harm, as the evaluation of their pharmacological profiles revealed lower potencies and/or efficacies. Conceived as a resource to foster collaborative investigation of the physiological effects of SCRAs, the library obtained can contribute to addressing the challenge posed by recreational designer drugs.
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.biopha.2023.114934
dc.identifier.eissn1950-6007
dc.identifier.issn0753-3322
dc.identifier.urihttps://doi.org/10.1016/j.biopha.2023.114934
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/92060
dc.identifier.wosidWOS:001009206600001
dc.language.isoen
dc.revistaBiomedicine & pharmacotherapy
dc.rightsacceso restringido
dc.subjectSynthetic cannabinoid receptor agonists
dc.subjectSCRAs
dc.subjectSynthetic cannabinoids NPS
dc.subjectAbuse drugs
dc.subjectDesigner drugs
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titlePharmacological insights emerging from the characterization of a large collection of synthetic cannabinoid receptor agonists designer drugs
dc.typeartículo
dc.volumen164
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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