Journal
LIFE-BASEL
Volume 10, Issue 12, Pages -Publisher
MDPI
DOI: 10.3390/life10120333
Keywords
endocannabinoids system; cannabinoid receptor type 2; cannabinoid receptor type 1; positive allosteric modulator; microglial cell; glutamate release
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Funding
- Italian Ministry of Health [2016-NET-2016-02363765]
- Fism-Fondazione Italiana Sclerosi Multipla [2017/R/16]
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Preclinical studies highlighted that compounds targeting cannabinoid receptors could be useful for developing novel therapies against neurodegenerative disorders. However, the chronic use of orthosteric agonists alone has several disadvantages, limiting their usefulness as clinically relevant drugs. Positive allosteric modulators might represent a promising approach to achieve the potential therapeutic benefits of orthosteric agonists of cannabinoid receptors through increasing their activity and limiting their adverse effects. The aim of the present study was to show the effects of positive allosteric ligands of cannabinoid receptors on the activity of a potent dual orthosteric agonist for neuroinflammation and excitotoxic damage by excessive glutamate release. The results indicate that the combination of an orthosteric agonist with positive allosteric modulators could represent a promising therapeutic approach to the treatment of neurodegenerative disorders.
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