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Ondelopran

From Wikipedia, the free encyclopedia
(Redirected fromLY-2196044)
Opioid antagonist acting at the mu, kappa and delta receptors
Ondelopran
Names
IUPAC name
6-[2-Fluoro-4-[[2-(oxan-4-yl)ethylamino]methyl]phenoxy]pyridine-3-carboxamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
KEGG
UNII
  • InChI=1S/C20H24FN3O3/c21-17-11-15(12-23-8-5-14-6-9-26-10-7-14)1-3-18(17)27-19-4-2-16(13-24-19)20(22)25/h1-4,11,13-14,23H,5-10,12H2,(H2,22,25)
    Key: QWNDOCKIKKQJNN-UHFFFAOYSA-N
  • C1COCCC1CCNCC2=CC(=C(C=C2)OC3=NC=C(C=C3)C(=O)N)F
Properties
C20H24FN3O3
Molar mass373.428 g·mol−1
Pharmacology
N07BB06 (WHO)
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

Ondelopran (LY-2196044) is an experimental drug being investigated for the treatment of alcoholism.[1]

Mechanism of action

[edit]

Ondelopran appears to be anantagonist atopioid receptors,[2] which means it blocks the action of other opioids (including endogenous opioids like endorphins) by preventing them from binding to the receptor. It antagonizes the three primary opioid receptors with potency of 0.4 (mu), 0.6 (kappa), and 1.9 nM (delta).[3]

Potential use

[edit]

A study has shown that treatment with ondelopran reduces the amount of alcohol intake (significantly more than in the placebo group), which means it could be a good path for the treatment of alcoholism.[4] Another test also displays more results which go in the same conclusion.[3]

References

[edit]
  1. ^"ClinicalTrials.gov".clinicaltrials.gov. 20 May 2019. Retrieved2024-08-22.
  2. ^Hillemacher, Thomas; Heberlein, Annemarie; Muschler, Marc An; Bleich, Stefan; Frieling, Helge (August 2011)."Opioid modulators for alcohol dependence".Expert Opinion on Investigational Drugs.20 (8):1073–1086.doi:10.1517/13543784.2011.592139.ISSN 1744-7658.PMID 21651459.
  3. ^abShagiakhmetov, Farid; Mukhametshina Elvira; Samsonov Mikhail (2019)."Novel triple opioid receptor antagonist ondelopran (LY2196044) for the treatment of alcohol dependence. Phase III study: female subjects subset efficacy and safety analysis".doi:10.13140/RG.2.2.35480.96001.{{cite journal}}:Cite journal requires|journal= (help)
  4. ^Wong, Conrad J.; Witcher, Jennifer; Mallinckrodt, Craig; Dean, Robert A.; Anton, Raymond F.; Chen, Yunfei; Fijal, Bonnie A.; Ouyang, Haojun; Dharia, Sweta; Sundseth, Scott S.; Schuh, Kory J.; Kinon, Bruce J. (February 2014)."A phase 2, placebo-controlled study of the opioid receptor antagonist LY2196044 for the treatment of alcohol dependence".Alcoholism: Clinical and Experimental Research.38 (2):511–520.doi:10.1111/acer.12257.ISSN 1530-0277.PMID 24010675.
Treatment ofdrug dependence (N07B)
Nicotine dependence
Alcohol dependence
Opioid dependence
Benzodiazepine dependence
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others
Retrieved from "https://en.wikipedia.org/w/index.php?title=Ondelopran&oldid=1276240672"
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