Targeting cannabinoid CB2 receptors in the Central Nervous System. Medicinal chemistry approaches and focus on neurodegenerative disorders affecting movement

Endocannabinoids activate two types of specific G-protein-coupled receptors (GPCRs), namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 receptors appear as prom...

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Detalhes bibliográficos
Autores: Navarro Brugal, Gemma, Morales, Paula, Rodríguez Cueto, Carmen, Fernández-Ruiz, Javier, Jagerovic, Nadine, Franco Fernández, Rafael
Tipo de documento: artigo
Estado:Versão publicada
Data de publicação:2016
País:España
Recursos:Universidad de Barcelona
Repositório:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/122089
Acesso em linha:https://hdl.handle.net/2445/122089
Access Level:Acceso aberto
Palavra-chave:Malalties neurodegeneratives
Receptors cel·lulars
Neurodegenerative Diseases
Cell receptors
Descrição
Resumo:Endocannabinoids activate two types of specific G-protein-coupled receptors (GPCRs), namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 receptors appear as promising drugs to combat CNS diseases (Parkinson's disease, Huntington's chorea, cerebellar ataxia, amyotrohic lateral sclerosis). Differential localization of CB2 receptors in neural cell types and upregulation in neuroinflammation are keys to understand the therapeutic potential in inter alia diseases that imply progressive neurodegeneration. Medicinal chemistry approaches are now engaged to develop imaging tools to map receptors in the living human brain, to develop more efficacious agonists, and to investigate the possibility to develop allosteric modulators.