Asimadolin

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	179340
ChEMBL	CHEMBL304542
Hemijski podaci
Formula	C27H30N2O2
Mol. masa	414.539 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C27H30N2O2/c1-28(25(21-11-5-2-6-12-21)20-29-18-17-24(30)19-29)27(31)26(22-13-7-3-8-14-22)23-15-9-4-10-16-23/h2-16,24-26,30H,17-20H2,1H3/t24-,25+/m0/s1 ; Key: JHLHNYVMZCADTC-LOSJGSFVSA-N
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 | uredi kod]

Literatura[uredi | uredi kod]

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ 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.
↑ 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.
↑ 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 | uredi kod]

	Portal Medicina
	Portal Hemija

[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

[pmid15989506-4] 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.

[pmid18715494-5] 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.

[pmid15233705-6] 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.

[pmid17900994-7] 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.

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Asimadolin

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