Cannabinor Explained
Cannabinor (PRS-211,375) is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist.[1] [2] It is classed as a "nonclassical" cannabinoid with a chemical structure similar to that of cannabidiol. It has a CB2 affinity of 17.4 nM vs 5,585 nM at CB1, giving it over 300× selectivity for CB2.[3] It showed analgesic effects in animal studies especially in models of neuropathic pain, but failed in Phase IIb human clinical trials due to lack of efficacy.[4]
See also
References
- Gratzke C, Streng T, Stief CG, Downs TR, Alroy I, Rosenbaum JS, Andersson KE, Hedlund P . Effects of cannabinor, a novel selective cannabinoid 2 receptor agonist, on bladder function in normal rats . European Urology . 57 . 6 . 1093–100 . June 2010 . 20207474 . 10.1016/j.eururo.2010.02.027 .
- Gratzke C, Streng T, Stief CG, Alroy I, Limberg BJ, Downs TR, Rosenbaum JS, Hedlund P, Andersson KE . 6 . Cannabinor, a selective cannabinoid-2 receptor agonist, improves bladder emptying in rats with partial urethral obstruction . The Journal of Urology . 185 . 2 . 731–6 . February 2011 . 21168864 . 10.1016/j.juro.2010.09.080 .
- Bow EW, Rimoldi JM . The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation . Perspectives in Medicinal Chemistry . 2016 . 8 . 17–39 . 27398024 . 10.4137/PMC.S32171 . 4927043 . free .
- Nevalainen T . Recent development of CB2 selective and peripheral CB1/CB2 cannabinoid receptor ligands . Current Medicinal Chemistry . 2013 . 21 . 2 . 187–203 . 24164198 . 10.2174/09298673113206660296 .