Википедија

SR-144,528

SR144528 je lek koji deluje kao potentan i visoko selektivan inverzni agonist CB2 receptora, sa Ki od 0,6 nM na CB2 i 400 nM na srodnom CB1 receptoru.[1][2] On se koristi u naučnim istraživanjima pri izučavanju funkcije CB2 receptora,[3][4][5] kao i za studiranje efekata CB1 receptora u izolaciji, jer mali broj CB1 agonista dostupan koji istovremeno nisu i CB2 agonisti.[6][7][8] On je isto tako inhibitor acil-koenzimA: holesterol aciltransferaze. To dejstvo je nezavisno od CB2 receptora.[9]

SR-144,528
IUPAC ime
N-[(1S)-endo-1,3,3-trimetilbiciklo [2.2.1]heptan2-il]-5-(4-hloro-3-metilfenil)-1-[(4-metilfenil)metil]-1H-pirazol-3-karboksamid
Identifikatori
CAS broj192703-06-3 ДаY
ATC kodnone
PubChemCID 3081355
ChEMBLCHEMBL381689 ДаY
Hemijski podaci
FormulaC29H34ClN3O
Molarna masa476,051
  • Cc5ccc(cc5)Cn3nc(cc3-c(cc2C)ccc2Cl)C(=O)NC1C(C)(C)C(C4)CCC14C

Reference уреди

  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 (1998). „SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor”. The Journal of Pharmacology and Experimental Therapeutics. 284 (2): 644—50. PMID 9454810. 
  2. ^ Portier M, Rinaldi-Carmona M, Pecceu F, Combes T, Poinot-Chazel C, Calandra B, Barth F, le Fur G, Casellas P (1999). „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. PMID 9918562. 
  3. ^ Gouldson P, Calandra B, Legoux P, Kernéis A, Rinaldi-Carmona M, Barth F, Le Fur G, Ferrara P, Shire D (2000). „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. PMID 10915832. doi:10.1016/S0014-2999(00)00439-8. 
  4. ^ 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”. Neuroscience. 119 (3): 747—57. PMID 12809695. doi:10.1016/S0306-4522(03)00126-X. 
  5. ^ Páldy E, Bereczki E, Sántha M, Wenger T, Borsodi A, Zimmer A, Benyhe S (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 International. 53 (6-8): 309—16. PMID 18804501. doi:10.1016/j.neuint.2008.08.005. 
  6. ^ Lay L, Angus JA, Wright CE (2000). „Pharmacological characterisation of cannabinoid CB(1) receptors in the rat and mouse”. European Journal of Pharmacology. 391 (1-2): 151—61. PMID 10720647. doi:10.1016/S0014-2999(00)00062-5. 
  7. ^ Germanò MP, D'Angelo V, Mondello MR, Pergolizzi S, Capasso F, Capasso R, Izzo AA, Mascolo N, De Pasquale R (2001). „Cannabinoid CB1-mediated inhibition of stress-induced gastric ulcers in rats”. Naunyn-Schmiedeberg's Archives of Pharmacology. 363 (2): 241—4. PMID 11218077. 
  8. ^ Abalo R, Cabezos PA, Vera G, Fernández-Pujol R, Martín MI (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 Society. 22 (6): 694—e206. PMID 20132133. doi:10.1111/j.1365-2982.2009.01466.x. 
  9. ^ Thewke D, Freeman-Anderson N, Pickle T, Netherland C, Chilton C (2009). „AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors”. Biochemical and Biophysical Research Communications. 381 (2): 181—6. PMC 2665256  . PMID 19338772. doi:10.1016/j.bbrc.2009.02.020. 

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