Asimadolin

Asimadolin
IUPAC ime
	N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
Identifikatori
CAS broj	153205-46-0
ATC kod	none
PubChem	CID 179340
ChEMBL	CHEMBL304542
Hemijski podaci
Formula	C27H30N2O2
Molarna masa	414.539 g/mol
	SMILES CN([C@H](CN1CC[C@@H](C1)O)C2=CC=CC=C2)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4; ;

Asimadolin (EMD-61753) je lek koji deluje kao periferni selektivni agonist κ-opioidnog receptora.^[1]^[2] 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.^[3]^[4]

Sinteza

Literatura

^ Barber A, Gottschlich R (1997). „Novel developments with selective, non-peptidic kappa-opioid receptor agonists”. Expert Opinion on Investigational Drugs. 6 (10): 1351—68. PMID 15989506. doi:10.1517/13543784.6.10.1351.
^ Camilleri M (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. PMC 2698012 . PMID 18715494. doi:10.1111/j.1365-2982.2008.01183.x.
^ Delvaux M, Beck A, Jacob J, Bouzamondo H, Weber FT, Frexinos J (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. PMID 15233705. doi:10.1111/j.1365-2036.2004.01922.x.
^ Szarka LA, Camilleri M, Burton D, Fox JC, McKinzie S, Stanislav T, Simonson J, Sullivan N, Zinsmeister AR (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. PMC 2128734 . PMID 17900994. doi:10.1016/j.cgh.2007.07.011.

Spoljašnje veze

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[pmid15989506-1] Barber A, Gottschlich R (1997). „Novel developments with selective, non-peptidic kappa-opioid receptor agonists”. Expert Opinion on Investigational Drugs. 6 (10): 1351—68. PMID 15989506. doi:10.1517/13543784.6.10.1351.

[pmid18715494-2] Camilleri M (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. PMC 2698012 . PMID 18715494. doi:10.1111/j.1365-2982.2008.01183.x.

[pmid15233705-3] Delvaux M, Beck A, Jacob J, Bouzamondo H, Weber FT, Frexinos J (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. PMID 15233705. doi:10.1111/j.1365-2036.2004.01922.x.

[pmid17900994-4] Szarka LA, Camilleri M, Burton D, Fox JC, McKinzie S, Stanislav T, Simonson J, Sullivan N, Zinsmeister AR (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. PMC 2128734 . PMID 17900994. doi:10.1016/j.cgh.2007.07.011.

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