Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation.

ABSTRACT: The potential, multifaceted therapeutic profile of cannabidiol (CBD), a major constituent derived from the Cannabis sativa plant, covers a wide range of neurological and psychiatric disorders, ranging from anxiety to pediatric epilepsy and drug addiction. However, the molecular targets responsible for these effects have been only partially identified. In this view, the involvement of the orexin system, the key regulator in arousal and the sleep/wake cycle, and in motivation and reward processes, including drug addiction, prompted us to explore, using computational and experimental approaches, the possibility that CBD could act as a ligand of orexin receptors, orexin 1 receptor of type 1 (OX1R) and type 2 (OX2R). Ligand-binding assays showed that CBD is a selective ligand of OX1R in the low

SUBMITTER: Vitale RM 

PROVIDER: S-EPMC8394412 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature