Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.

GPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focuse...

Descripción completa

Detalles Bibliográficos
Autores: Figuerola Asencio, Laura, Morales, Paula, Zhao, Pingwei, Hurst, Dow P, Sayed, Sommayah S, Colón, Katsuya L, Gómez Cañas, María, Fernández Ruiz, José Javier, Croatt, Mitchell P, Reggio, Patricia H, Abood, Mary E, Jagerovic, Nadine
Tipo de recurso: artículo
Fecha de publicación:2023
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/133311
Acceso en línea:https://hdl.handle.net/20.500.14352/133311
Access Level:acceso abierto
Palabra clave:GPR55
Antagonist
Cannabinoid
Thienopyrimidine
SAR
Ciencias Biomédicas
Farmacología (Medicina)
24 Ciencias de la Vida
Descripción
Sumario:GPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focused on a thienopyrimidine scaffold based on the GPR55 antagonist ML192, previously discovered by high-throughput screening. The GPR55 activities of the new synthesized compounds were assessed using β-arrestin recruitment assays in Chinese hamster ovary cells overexpressing human GPR55. Some derivatives were identified as GPR55 antagonists with functional efficacy and selectivity versus CB1 and CB2 cannabinoid receptors.

Similares en LA Referencia