Pancreatic stellate cells. The cells in the lower frame are under the action of WIN 55,212-2. They are thought to assume a more "quiescent" phenotype. From Michalski et al., 2008.[2]
WIN 55,212-2 is a potent cannabinoidreceptor agonist[6] that has been found to be a potent analgesic[7] in a rat model of neuropathic pain.[8] It activatesp42 andp44MAP kinase via receptor-mediated signaling.[9]
WIN 55,212-2, along withHU-210 andJWH-133, may prevent the inflammation caused byamyloid beta proteins involved inAlzheimer's disease, in addition to preventing cognitive impairment and loss of neuronalmarkers. This anti-inflammatory action is induced through agonist action atcannabinoid receptors, which preventsmicroglial activation that elicits the inflammation.
WIN 55,212-2 is a full agonist at theCB1 cannabinoid receptor (Ki = 1.9 nM) and has much higher affinity thanTHC (Ki = 41 nM) for this receptor.[11] WIN 55,212-2 is also an agonist of thePPARα andPPARγ nuclear receptors.[12]
WIN 55,212-2 reduces voluntary wheel running in laboratory mice, but with effects that depend on both genetic background and sex.[13]
In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as WIN 55,212-2 areSchedule I Controlled Substances.[14] WIN 55,212-2 is illegal in the UK.[15]
^Compton DR, Gold LH, Ward SJ, Balster RL, Martin BR (December 1992). "Aminoalkylindole analogs: cannabimimetic activity of a class of compounds structurally distinct from delta 9-tetrahydrocannabinol".The Journal of Pharmacology and Experimental Therapeutics.263 (3):1118–1126.PMID1335057.
^Zhang Q, Ma P, Iszard M, Cole RB, Wang W, Wang G (October 2002). "In vitro metabolism of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]1,4-benzoxazinyl]-(1-naphthalenyl) methanone mesylate, a cannabinoid receptor agonist".Drug Metabolism and Disposition.30 (10):1077–1086.doi:10.1124/dmd.30.10.1077.PMID12228183.S2CID10848076.
^Felder CC, Joyce KE, Briley EM, Mansouri J, Mackie K, Blond O, et al. (September 1995). "Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors".Molecular Pharmacology.48 (3):443–450.PMID7565624.
^Herzberg U, Eliav E, Bennett GJ, Kopin IJ (January 1997). "The analgesic effects of R(+)-WIN 55,212-2 mesylate, a high affinity cannabinoid agonist, in a rat model of neuropathic pain".Neuroscience Letters.221 (2–3):157–160.doi:10.1016/S0304-3940(96)13308-5.PMID9121688.S2CID33643599.
^Kuster JE, Stevenson JI, Ward SJ, D'Ambra TE, Haycock DA (March 1993). "Aminoalkylindole binding in rat cerebellum: selective displacement by natural and synthetic cannabinoids".The Journal of Pharmacology and Experimental Therapeutics.264 (3):1352–1363.PMID8450470.
^Keeney BK, Meek TH, Middleton KM, Holness LF, Garland T (June 2012). "Sex differences in cannabinoid receptor-1 (CB1) pharmacology in mice selectively bred for high voluntary wheel-running behavior".Pharmacology, Biochemistry, and Behavior.101 (4):528–537.doi:10.1016/j.pbb.2012.02.017.PMID22405775.S2CID25174208.
^González C, Herradón E, Abalo R, Vera G, Pérez-Nievas BG, Leza JC, et al. (May 2011). "Cannabinoid/agonist WIN 55,212-2 reduces cardiac ischaemia–reperfusion injury in Zucker diabetic fatty rats: role of CB2 receptors and iNOS/eNOS".Diabetes/Metabolism Research and Reviews.27 (4):331–340.doi:10.1002/dmrr.1176.PMID21309057.S2CID32450365.
^Shmist YA, Goncharov I, Eichler M, Shneyvays V, Isaac A, Vogel Z, Shainberg A (February 2006). "Delta-9-tetrahydrocannabinol protects cardiac cells from hypoxia via CB2 receptor activation and nitric oxide production".Molecular and Cellular Biochemistry.283 (1–2):75–83.doi:10.1007/s11010-006-2346-y.PMID16444588.S2CID24074568.
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