Cannabidiol skews biased agonism at cannabinoid CB1 and CB2 receptors with smaller effect in CB1-CB2 heteroreceptor complexes

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Navarro, Gemma; Reyes-Resina, I.; Rivas-Santisteban, R.; Sánchez de Medina, V.; Morales, Paula; Casano, S.; Ferreiro-Vera, C.; Lillo, A.; Aguinaga, D.; Jagerovic, Nadine; Nadal, X.; Franco, R.; (2018)
  • Journal: Biochemical Pharmacology 157: 148-158 (2018) (issn: 0006-2952, eissn: 1873-2968)
  • Related identifiers: doi: 10.1016/j.bcp.2018.08.046, handle: 10261/173912
  • Subject: BRET | CNS | Drug discovery | Endocannabinoids | Phytocannabinoids | G-protein-coupled receptor

Currently, biased agonism is at the center stage of drug development approaches. We analyzed effects of a battery of cannabinoids plus/minus cannabidiol (CBD) in four functional parameters (cAMP levels, phosphorylation of extracellular signal–regulated kinases (ERK1/2),... View more
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