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The Solution to the Medicinal Cannabis Problem
Published in Michael E. Schatman, Ethical Issues in Chronic Pain Management, 2016
Ajulemic acid (CT-3) is synthetic cannabinoid derivative with analgesic and anti-inflammatory properties in animal models (64,65) that have advanced to Phase II clinical trials. Ajulemic acid binds to the peroxisome proliferator-activated receptor gamma, involved in inflammatory mechanisms (66), and also suppresses monocyte interleukin-1beta production in vitro (67). Ajulemic acid seems to have promising anti-inflammatory and analgesic properties, but recent reports suggest that this agent does bind to CB1, and could produce psychoactive effects (68). Clinical research is currently confined to treatment of interstitial cystitis.
The Role of Cannabis and Cannabinoids in Pain Management
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Ajulemic acid is a synthetic derived from delta-8-THC that does not bind to cannabinoid receptors. CT3 was developed by Atlantic Pharmaceuticals. It has shown analgesic and anti-inflammatory properties in animal models without COX-1 inhibition side effects (S. H. Burstein, 2000, 2001). It has shown strong analgesic and antiinflammatory properties in animal models of arthritis without COX-1 inhibition side effects such as ulcer production, and is in advanced clinical trials (S. H. Burstein 2000, 2001). Ajulemic acid binds to the peroxisome proliferator-activated receptor gamma, part of the nuclear receptor superfamily involved in inflammatory processes (Liu, Li, Burstein, Zurier, & Chen, 2003), and also suppresses human monocyte interleukin-1beta production in vitro (Zurier, Rossetti, Burstein, & Bidinger, 2003). Ajulemic acid may represent a valuable addition to cannabinoid pharmaceuticals used for anti-inflammatory and analgesic effects.
The potential role of cannabinoids in dermatology
Published in Journal of Dermatological Treatment, 2020
Tabrez Sheriff, Matthew J. Lin, Danielle Dubin, Hooman Khorasani
The CB1 and CB2 receptors may modulate the fibrotic response in conditions such as systemic sclerosis, morphoea, and drug-induced fibrosis. Specifically, CB2 activation in models of fibrotic dermal tissue modulated the immune response, which prevented cutaneous fibrosis and tissue leucocyte infiltration (42). Investigation of a synthetic CB2 agonist in mice with bleomycin-induced fibrosis was also associated with reduced dermal thickening and leucocyte infiltration, suggesting that CB2 receptors may be targeted in the early inflammatory phase of systemic sclerosis (42). This was supported by Gonzalez et al. who identified Ajulemic acid, another nonpsychoactive synthetic analog of THC, which significantly prevented fibrosis in bleomycin exposed mice by stimulating PPAR43).
Medical cannabis and cannabinoids in rheumatology: where are we now?
Published in Expert Review of Clinical Immunology, 2019
Piercarlo Sarzi-Puttini, Alberto Batticciotto, Fabiola Atzeni, Laura Bazzichi, Manuela Di Franco, Fausto Salaffi, Daniela Marotto, Angela Ceribelli, Jacob N Ablin, Winfred Hauser
A recent study has found that plasma 2-AG levels are significantly higher in SLE patients than in healthy subjects (p = 0.0059). and that the patients with the highest levels had less active disease; there were no between-group differences in the concentrations of N-arachidonoylethanolamine (AEA) or its congeners N-palmitoylethanolamine (PEA) and N-oleoylethanolamine (OEA). A gene expression analysis of metabolic enzymes and the receptor targets of eCBs, and an investigation of the functional activity and protein expression of selected components of the eCB system, revealed that the expression and functional activity of the 2-AG biosynthetic enzyme DAGL were selectively enhanced in the PBMCs of the patients. This study demonstrates for the first time that SLE patients have an altered ECS [64], and it is interesting to note that modulating CBr2 expression certainly provides a biochemical and molecular basis justifying a planned phase II clinical trial (NCT03093402) designed to evaluate the efficacy, safety and tolerability of a new and highly purified composition of ajulemic acid (a synthetic non-psychoactive cannabinoid) in SLE patients [65].
In quest of a new therapeutic approach in COVID-19: the endocannabinoid system
Published in Drug Metabolism Reviews, 2021
Ondine Lucaciu, Ovidiu Aghiorghiesei, Nausica Bianca Petrescu, Ioana Codruta Mirica, Horea Rareș Ciprian Benea, Dragoș Apostu
PPAR receptor pathway is downregulated by CBD in LPS-treated mice (Pisanti et al. 2017). Multiple cannabinoids activate the PPARγ such as anandamide, 2-arachidonoylglycerol, ajulemic acid, JU 210, and others (O'Sullivan and Kendall 2010; Mamber et al. 2020) (Figure 5).