2013
DOI: 10.1371/journal.pone.0062511
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Effects on Immune Cells of a New 1,8-Naphthyridin-2-One Derivative and Its Analogues as Selective CB2 Agonists: Implications in Multiple Sclerosis

Abstract: The efficacy of cannabinoids in the treatment of multiple sclerosis is widely documented; however their use is limited by psychoactivity mainly ascribed to the activation of the cannabinoid receptor CB1. Emerging findings support as alternative strategy in the treatment of neurodegenerative disorders, the application of compounds targeting the CB2 receptor, since likely unrelated to these side effects. Recently, a novel class of compounds, 1,8-naphthyridine, pyridine and quinoline derivatives have been demonst… Show more

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Cited by 27 publications
(19 citation statements)
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“…Furthermore, studies performed in animals with experimental autoimmune encephalomyelitis (EAE), an MS model, showed that cannabinoids ameliorate symptoms (spasticity, tremor, ataxia and pain), reduce inflammation and favour remyelination via CB 1 ‐ and CB 2 ‐mediated mechanisms . Finally, most immunomodulatory/anti‐inflammatory activities of cannabinoids in peripheral blood mononuclear cells (PBMCs) are mediated through CB 2 receptors .…”
Section: Introductionmentioning
confidence: 99%
“…Furthermore, studies performed in animals with experimental autoimmune encephalomyelitis (EAE), an MS model, showed that cannabinoids ameliorate symptoms (spasticity, tremor, ataxia and pain), reduce inflammation and favour remyelination via CB 1 ‐ and CB 2 ‐mediated mechanisms . Finally, most immunomodulatory/anti‐inflammatory activities of cannabinoids in peripheral blood mononuclear cells (PBMCs) are mediated through CB 2 receptors .…”
Section: Introductionmentioning
confidence: 99%
“…Interestingly the CB2R, but not the CB1R, was reported to be upregulated in activated microglial cells and peripheral macrophages in EAE model of MS [ 85 ], and was demonstrated to have critical roles in inhibiting leukocyte/endothelial interactions and attenuating infiltration of inflammatory cells [ 576 ]. Additionally, CB2R-selective agonists were shown to exert potent anti-inflammatory and anti-proliferative effects on immune cells isolated from MS patients [ 577 , 578 ]. WIN-55,212-2 was reported to reduce inflammatory infiltrates in spinal cord and also induced apoptosis of encephalitogenic T-cell populations, partially via the CB2R in EAE model [ 579 ].…”
Section: Biological Role Of the Cannabinoid Receptorsmentioning
confidence: 99%
“…In fact, 1, 8-naphthyridine-2-one derivative reduces the levels of the Cox-2 enzyme in lymphocytes. [86]. He also develops cycloheptyl substituted derivative VL15 (78) as a selective CB2 receptor agent with high selectivity and affinity at the CB2 receptor and havening excellent protective role of this receptor in various neurological diseases with an autoimmune constituent like multiple sclerosis with immunomodulatory activity [87].…”
Section: Cb2 Receptor Agonists With Anticancer and Immunomodulatory Amentioning
confidence: 99%