Journal
EXPERT OPINION ON DRUG DISCOVERY
Volume 15, Issue 8, Pages 917-930Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/17460441.2020.1752178
Keywords
Cannabinoid; allosteric; bias; peripheral; mitochondrial; multitarget; off-target
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Funding
- Ministry of Science, Innovation, and Universities, Spain (MCIU)/FEDER [RTI2018-095544-B-I00]
- Spanish National Research Council (CSIC) [PIE-201580E033]
- National Institutes of Health [R01 DA0455698-01]
- Comunidad de Madrid (CM) programme 'Attraccion de Talentos' [2018-T28MD-10819]
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Introduction: 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, CB1 and CB2, along with inhibitors of the endocannabinoid enzymes have been thoroughly studied in diverse disease models. In fact, phytocannabinoids such as cannabidiol or Delta(9)-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 CB1 and CB2 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.
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