Chemistry:SR-144,528
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Short description: Chemical compound
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| Formula | C29H34ClN3O |
| Molar mass | 476.06 g·mol−1 |
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SR144528 is a drug that acts as a potent and highly selective CB2 receptor inverse agonist, with a Ki 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
References
- ↑ "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. PMID 9454810. http://jpet.aspetjournals.org/content/284/2/644.long.
- ↑ "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. PMID 9918562. http://jpet.aspetjournals.org/content/288/2/582.long.
- ↑ "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. doi:10.1016/S0014-2999(00)00439-8. PMID 10915832.
- ↑ "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. doi:10.1016/S0306-4522(03)00126-X. PMID 12809695.
- ↑ "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. doi:10.1016/j.neuint.2008.08.005. PMID 18804501.
- ↑ "Cannabinoid Receptor 2 (CB 2 ) Signals via G-alpha-s and Induces IL-6 and IL-10 Cytokine Secretion in Human Primary Leukocytes" (in en). ACS Pharmacology & Translational Science 2 (6): 414–428. 2019-10-19. doi:10.1021/acsptsci.9b00049. ISSN 2575-9108. PMID 32259074.
- ↑ "Pharmacological characterisation of cannabinoid CB(1) receptors in the rat and mouse". European Journal of Pharmacology 391 (1–2): 151–61. March 2000. doi:10.1016/S0014-2999(00)00062-5. PMID 10720647.
- ↑ "Cannabinoid CB1-mediated inhibition of stress-induced gastric ulcers in rats". Naunyn-Schmiedeberg's Archives of Pharmacology 363 (2): 241–4. February 2001. doi:10.1007/s002100000360. PMID 11218077.
- ↑ "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. doi:10.1111/j.1365-2982.2009.01466.x. PMID 20132133.
- ↑ "AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors". Biochemical and Biophysical Research Communications 381 (2): 181–6. April 2009. doi:10.1016/j.bbrc.2009.02.020. PMID 19338772.
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