SR-144,528

Из Википедије, слободне енциклопедије
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
Klinički podaci
Identifikatori
CAS broj 192703-06-3
ATC kod nije dodeljen
PubChem[1][2] 3081355
ChEMBL[3] CHEMBL381689 YesY
Hemijski podaci
Formula C29H34ClN3O 
Mol. masa 476,051
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

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.[4][5] On se koristi u naučnim istraživanjima pri izučavanju funkcije CB2 receptora,[6][7][8] kao i za studiranje efekata CB1 receptora u izolaciji, jer mali broj CB1 agonista dostupan koji istovremeno nisu i CB2 agonisti.[9][10][11] On je isto tako inhibitor acil-koenzimA: holesterol aciltransferaze. To dejstvo je nezavisno od CB2 receptora.[12]

Reference[уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  4. 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 (February 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. 
  5. Portier M, Rinaldi-Carmona M, Pecceu F, Combes T, Poinot-Chazel C, Calandra B, Barth F, le Fur G, Casellas P (February 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. 
  6. Gouldson P, Calandra B, Legoux P, Kernéis A, Rinaldi-Carmona M, Barth F, Le Fur G, Ferrara P, Shire D (July 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. DOI:10.1016/S0014-2999(00)00439-8. PMID 10915832. 
  7. 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. DOI:10.1016/S0306-4522(03)00126-X. PMID 12809695. 
  8. Páldy E, Bereczki E, Sántha M, Wenger T, Borsodi A, Zimmer A, Benyhe S (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 International 53 (6-8): 309–16. DOI:10.1016/j.neuint.2008.08.005. PMID 18804501. 
  9. Lay L, Angus JA, Wright CE (March 2000). „Pharmacological characterisation of cannabinoid CB(1) receptors in the rat and mouse”. European Journal of Pharmacology 391 (1-2): 151–61. DOI:10.1016/S0014-2999(00)00062-5. PMID 10720647. 
  10. Germanò MP, D'Angelo V, Mondello MR, Pergolizzi S, Capasso F, Capasso R, Izzo AA, Mascolo N, De Pasquale R (February 2001). „Cannabinoid CB1-mediated inhibition of stress-induced gastric ulcers in rats”. Naunyn-Schmiedeberg's Archives of Pharmacology 363 (2): 241–4. PMID 11218077. 
  11. Abalo R, Cabezos PA, Vera G, Fernández-Pujol R, Martín MI (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 Society 22 (6): 694–e206. DOI:10.1111/j.1365-2982.2009.01466.x. PMID 20132133. 
  12. Thewke D, Freeman-Anderson N, Pickle T, Netherland C, Chilton C (April 2009). „AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors”. Biochemical and Biophysical Research Communications 381 (2): 181–6. DOI:10.1016/j.bbrc.2009.02.020. PMC 2665256. PMID 19338772. 

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