SR144528 is a drug that acts as a potent and highly selective CB2receptorinverse agonist, with a Ki of 0.6nM at CB2 and 400nM at the related CB1 receptor. It is used in scientific research for investigating the function of the CB2 receptor, as well as for studying the effects of CB1 receptors in isolation, as few CB1 agonists that do not also show significant activity as CB2 agonists are available. It has also been found to be an inhibitor of acyl-coenzymeA:cholesterol acyltransferase, an effect that appears to be independent from its action on CB2 receptors.
^Rinaldi-Carmona M et al. (February 1998). "SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor". The Journal of Pharmacology and Experimental Therapeutics284 (2): 644–50. PMID9454810.CS1 maint: Explicit use of et al. (link)
^Portier M et al. (February 1999). "SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist". The Journal of Pharmacology and Experimental Therapeutics288 (2): 582–9. PMID9918562.CS1 maint: Explicit use of et al. (link)
^Gouldson P et al. (July 2000). "Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor". European Journal of Pharmacology401 (1): 17–25. doi:10.1016/S0014-2999(00)00439-8. PMID10915832.CS1 maint: Explicit use of et al. (link)
^Nackley AG, Makriyannis A, Hohmann AG (2003). "Selective activation of cannabinoid CB(2) receptors suppresses spinal fos protein expression and pain behavior in a rat model of inflammation". Neuroscience119 (3): 747–57. doi:10.1016/S0306-4522(03)00126-X. PMID12809695.
^Páldy E et al. (December 2008). "CB(2) cannabinoid receptor antagonist SR144528 decreases mu-opioid receptor expression and activation in mouse brainstem: role of CB(2) receptor in pain". Neurochemistry International53 (6-8): 309–16. doi:10.1016/j.neuint.2008.08.005. PMID18804501.CS1 maint: Explicit use of et al. (link)
^Lay L, Angus JA, Wright CE (March 2000). "Pharmacological characterisation of cannabinoid CB(1) receptors in the rat and mouse". European Journal of Pharmacology391 (1-2): 151–61. doi:10.1016/S0014-2999(00)00062-5. PMID10720647.
^Germanò MP et al. (February 2001). "Cannabinoid CB1-mediated inhibition of stress-induced gastric ulcers in rats". Naunyn-Schmiedeberg's Archives of Pharmacology363 (2): 241–4. doi:10.1007/s002100000360. PMID11218077.CS1 maint: Explicit use of et al. (link)
^Abalo R et al. (June 2010). "The cannabinoid antagonist SR144528 enhances the acute effect of WIN 55,212-2 on gastrointestinal motility in the rat". Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society22 (6): 694–e206. doi:10.1111/j.1365-2982.2009.01466.x. PMID20132133.CS1 maint: Explicit use of et al. (link)