GW-405,833

Iz Wikipedije, slobodne enciklopedije
Idi na navigaciju Idi na pretragu
GW-405,833
(IUPAC) ime
1-(2,3-Dihlorobenzoil)-5-metoksi-2-metil-3-[2-(4-morfolinil)etil]-1H-indol
Klinički podaci
Identifikatori
CAS broj 180002-83-9
ATC kod nije dodeljen
PubChem[1][2] 9911463
ChEMBL[3] CHEMBL73711 YesY
Hemijski podaci
Formula C23H24Cl2N2O3 
Mol. masa 447,353 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

GW-405,833 (L-768,242) je lek koji deluje kao potentan i selektivan parcijalni agonist kanabinoidnog receptora CB2, sa EC50 vrednošću od 0,65 nM i selektivnošću od oko 1200x za CB2 u odnosu na CB1 receptor.[4][5] Ispitivanja na životinjama su pokazala da ima antiinflamatorno antihiperalgetsko dejstvo pri niskim dozama, čemu sledi ataksija i analgetičko dejstvo pri povišenju doze.[6][7] Selektivni CB2 agonisti poput GW-405,833 mogu potencijalno do budu korisni u tretmanu alodinije i neuropatičkog bola za koji su drugi lekove nepodesni.[8][9]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. Huffman JW. The search for selective ligands for the CB2 receptor. Current Pharmaceutical Design. 2000 Sep;6(13):1323-37. DOI:10.2174/1381612003399347 PMID 10903395
  5. Marriott KS, Huffman JW. Recent advances in the development of selective ligands for the cannabinoid CB(2) receptor. Current Topics in Medicinal Chemistry. 2008;8(3):187-204. DOI:10.2174/156802608783498014 PMID 18289088
  6. Clayton N, Marshall FH, Bountra C, O'Shaughnessy CT. CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain. Pain. 2002 Apr;96(3):253-60. PMID 11972997
  7. Valenzano KJ, Tafesse L, Lee G, Harrison JE, Boulet JM, Gottshall SL, Mark L, Pearson MS, Miller W, Shan S, Rabadi L, Rotshteyn Y, Chaffer SM, Turchin PI, Elsemore DA, Toth M, Koetzner L, Whiteside GT. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48(5):658-72. PMID 15814101
  8. Beltramo M, Bernardini N, Bertorelli R, Campanella M, Nicolussi E, Fredduzzi S, Reggiani A. CB2 receptor-mediated antihyperalgesia: possible direct involvement of neural mechanisms. European Journal of Neuroscience. 2006 Mar;23(6):1530-8. DOI:10.1111/j.1460-9568.2006.04684.x PMID 16553616
  9. Leichsenring A, Andriske M, Bäcker I, Stichel CC, Lübbert H. Analgesic and antiinflammatory effects of cannabinoid receptor agonists in a rat model of neuropathic pain. Naunyn Schmiedebergs Archives of Pharmacology. 2009 Jan 18. PMID 19152053

Spoljašnje veze[uredi - уреди | uredi izvor]