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Title

Novel approaches and current challenges with targeting the endocannabinoid system

AuthorsMorales, Paula ; Jagerovic, Nadine
KeywordsCannabinoid
Allosteric
Bias
Peripheral
Mitochondrial
Multitarget
Off-target
Issue Date2020
PublisherTaylor & Francis
CitationExpert Opinion on Drug Discovery (2020)
AbstractIntroduction: The pathophysiological relevance of the endocannabinoid system has been widely demonstrated in a variety of diseases including cancer, neurological disorders, and metabolic issues. Therefore, targeting the receptors and the endogenous machinery involved in this system can provide a successful therapeutic outcome. Ligands targeting the canonical cannabinoid receptors, CB and CB, along with inhibitors of the endocannabinoid enzymes have been thoroughly studied in diverse disease models. In fact, phytocannabinoids such as cannabidiol or Δ-tetrahydrocannabinol are currently on the market for the management of neuropathic pain due to spasticity in multiple sclerosis or seizures in children epilepsy amongst others. Areas covered: Challenges in the pharmacology of cannabinoids arise from its pharmacokinetics, off-target effects, and psychoactive effects. In this context, the current review outlines the novel molecular approaches emerging in the field discussing their clinical potential. Expert opinion: Even if orthosteric CB and CB ligands are on the forefront in cannabinoid clinical research, emerging strategies such as allosteric or biased modulation of these receptors along with controlled off-targets effects may increase the therapeutic potential of cannabinoids.
Publisher version (URL)http://dx.doi.org/10.1080/17460441.2020.1752178
URIhttp://hdl.handle.net/10261/216243
DOIhttp://dx.doi.org/10.1080/17460441.2020.1752178
Identifiersdoi: 10.1080/17460441.2020.1752178
issn: 1746-045X
Appears in Collections:(IQM) Artículos
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