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Asimadoline

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Asimadoline
Clinical data
Other namesEMD-61753
ATC code
  • none
Identifiers
  • N-[(1S)-2-[(3S)-3-Hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C27H30N2O2
Molar mass 414.549 g·mol−1
3D model (JSmol)
  • CN([C@H](CN1CC[C@@H](C1)O)C2=CC=CC=C2)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4
  • 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 checkY
  • Key:JHLHNYVMZCADTC-LOSJGSFVSA-N checkY
 NcheckY (what is this?)   (verify)

Asimadoline (EMD-61753) is an experimental drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist.[1] [2] Because of its low penetration across the blood–brain barrier, asimadoline lacks the psychotomimetic effects of centrally acting KOR agonists, and consequently was thought to have potential for medical use. It has been studied as a possible treatment for irritable bowel syndrome, with reasonable efficacy seen in clinical trials,[3] [4] but it has never been approved or marketed.

See also

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References

[edit ]
  1. ^ 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.
  2. ^ Camilleri M (September 2008). "Novel pharmacology: asimadoline, a kappa-opioid agonist, and visceral sensation". Neurogastroenterology & Motility. 20 (9): 971–9. doi:10.1111/j.1365-2982.2008.01183.x. PMC 2698012 . PMID 18715494.
  3. ^ 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. S2CID 23570291.
  4. ^ 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. 5 (11): 1268–75. doi:10.1016/j.cgh.2007年07月01日1. PMC 2128734 . PMID 17900994.
Drugs for
functional
bowel
disorders
Antimuscarinics
Tertiary
amino group
Quaternary
ammonium

compounds
Phosphodiesterase
inhibitors
Acting on
serotonin receptors
Other
Belladonna
and derivatives
(antimuscarinics)
Propulsives
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others

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