SR-144,528 explained

SR144528 is a drug that acts as a potent and highly selective CB₂ receptor inverse agonist, with a K_i of 0.6 nM at CB₂ and 400 nM at the related CB₁ receptor.^{[1] [2]} It is used in scientific research for investigating the function of the CB₂ receptor,^{[3] [4] [5] [6]} 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.^{[7] [8] [9]} It has also been found to be an inhibitor of sterol O-acyltransferase, an effect that appears to be independent from its action on CB₂ receptors.^[10]

See also

• NESS-040C5
• Rimonabant
• MN-25

Notes and References

1. Rinaldi-Carmona M, Barth F, Millan J, Derocq JM, Casellas P, Congy C, Oustric D, Sarran M, Bouaboula M, Calandra B, Portier M, Shire D, Brelière JC, Le Fur GL . 6 . SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor . The Journal of Pharmacology and Experimental Therapeutics . 284 . 2 . 644–50 . February 1998 . 9454810 .
2. Portier M, Rinaldi-Carmona M, Pecceu F, Combes T, Poinot-Chazel C, Calandra B, Barth F, le Fur G, Casellas P . 6 . SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist . The Journal of Pharmacology and Experimental Therapeutics . 288 . 2 . 582–9 . February 1999 . 9918562 .
3. Gouldson P, Calandra B, Legoux P, Kernéis A, Rinaldi-Carmona M, Barth F, Le Fur G, Ferrara P, Shire D . 6 . Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor . European Journal of Pharmacology . 401 . 1 . 17–25 . July 2000 . 10915832 . 10.1016/S0014-2999(00)00439-8 .
4. Nackley AG, Makriyannis A, Hohmann AG . Selective activation of cannabinoid CB(2) receptors suppresses spinal fos protein expression and pain behavior in a rat model of inflammation . Neuroscience . 119 . 3 . 747–57 . 4 July 2003 . 12809695 . 10.1016/S0306-4522(03)00126-X . 6447695 . Alexandros Makriyannis .
5. Páldy E, Bereczki E, Sántha M, Wenger T, Borsodi A, Zimmer A, Benyhe S . CB(2) cannabinoid receptor antagonist SR144528 decreases mu-opioid receptor expression and activation in mouse brainstem: role of CB(2) receptor in pain . Neurochemistry International . 53 . 6–8 . 309–16 . December 2008 . 18804501 . 10.1016/j.neuint.2008.08.005 . 22671432 .
6. Saroz Y, Kho DT, Glass M, Graham ES, Grimsey NL . 2019-10-19. Cannabinoid Receptor 2 (CB 2) Signals via G-alpha-s and Induces IL-6 and IL-10 Cytokine Secretion in Human Primary Leukocytes. ACS Pharmacology & Translational Science. 2. 6. en. 414–428. 10.1021/acsptsci.9b00049. 32259074. 7088898. 2575-9108. free.
7. Lay L, Angus JA, Wright CE . Pharmacological characterisation of cannabinoid CB(1) receptors in the rat and mouse . European Journal of Pharmacology . 391 . 1–2 . 151–61 . March 2000 . 10720647 . 10.1016/S0014-2999(00)00062-5 .
8. Germanò MP, D'Angelo V, Mondello MR, Pergolizzi S, Capasso F, Capasso R, Izzo AA, Mascolo N, De Pasquale R . 6 . Cannabinoid CB1-mediated inhibition of stress-induced gastric ulcers in rats . Naunyn-Schmiedeberg's Archives of Pharmacology . 363 . 2 . 241–4 . February 2001 . 11218077 . 10.1007/s002100000360 . 2655432 .
9. Abalo R, Cabezos PA, Vera G, Fernández-Pujol R, Martín MI . The cannabinoid antagonist SR144528 enhances the acute effect of WIN 55,212-2 on gastrointestinal motility in the rat . Neurogastroenterology and Motility . 22 . 6 . 694–e206 . June 2010 . 20132133 . 10.1111/j.1365-2982.2009.01466.x . 10520671 .
10. Thewke D, Freeman-Anderson N, Pickle T, Netherland C, Chilton C . AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors . Biochemical and Biophysical Research Communications . 381 . 2 . 181–6 . April 2009 . 19338772 . 2665256 . 10.1016/j.bbrc.2009.02.020 .