Asimadolin

Izvor: Wikipedia
Asimadolin
(IUPAC) ime
N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
Klinički podaci
Identifikatori
CAS broj 153205-46-0
ATC kod nije dodeljen
PubChem[1][2] 179340
ChEMBL[3] CHEMBL304542 YesY
Hemijski podaci
Formula C27H30N2O2 
Mol. masa 414.539 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Asimadolin (EMD-61753) je lek koji deluje kao periferni selektivni agonist κ-opioidnog receptora.[4][5] Zbog njegove neznatne sposobnosti prolaska kroz krvno moždanu barijeru, asimadolin ne ispoljava psihotomimetičke efekte centralno delujućih kapa agonista, i konsekventno ima veći potencijal za medicinsku upotrebu. On je bio testiran kao mogući treatman upalnu bolest creva, i utvrđeno je da je relativno efikasan.[6][7]

Sinteza[uredi - уреди]

Asimadoline.png

Literatura[uredi - 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. Barber A, Gottschlich R (October 1997). "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opinion on Investigational Drugs 6 (10): 1351–68. doi:10.1517/13543784.6.10.1351. PMID 15989506. 
  5. Camilleri M (September 2008). "Novel pharmacology: asimadoline, a kappa-opioid agonist, and visceral sensation". Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society 20 (9): 971–9. doi:10.1111/j.1365-2982.2008.01183.x. PMC 2698012. PMID 18715494. 
  6. Delvaux M, Beck A, Jacob J, Bouzamondo H, Weber FT, Frexinos J (July 2004). "Effect of asimadoline, a kappa opioid agonist, on pain induced by colonic distension in patients with irritable bowel syndrome". Alimentary Pharmacology & Therapeutics 20 (2): 237–46. doi:10.1111/j.1365-2036.2004.01922.x. PMID 15233705. 
  7. Szarka LA, Camilleri M, Burton D, Fox JC, McKinzie S, Stanislav T, Simonson J, Sullivan N, Zinsmeister AR (November 2007). "Efficacy of on-demand asimadoline, a peripheral kappa-opioid agonist, in females with irritable bowel syndrome". Clinical Gastroenterology and Hepatology : the Official Clinical Practice Journal of the American Gastroenterological Association 5 (11): 1268–75. doi:10.1016/j.cgh.2007.07.011. PMC 2128734. PMID 17900994. 

Spoljašnje veze[uredi - уреди]

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