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- LY-2459989 abstract "LY-2459989 is a silent antagonist of the κ-opioid receptor (KOR) that has been developed by Eli Lilly as a radiotracer (labeled with carbon-11) of the aforementioned receptor. It possesses high affinity for the KOR (Ki = 0.18 nM) and is highly selective for it over the μ-opioid receptor (Ki = 7.68 nM) and the δ-opioid receptor (Ki = 91.3 nM) (over 43-fold selectivity for the KOR over the other opioid receptors). LY-2459989 is a fluorine-containing analogue and follow-up compound of LY-2795050, the first-ever KOR-selective antagonist radiotracer. Relative to LY-2795050, LY-2459989 displays 4-fold higher affinity for the KOR and similar selectivity and also possesses greatly improved central nervous system permeation (brain levels were found to be 6-fold higher than those of LY-2795050). The drug appears to possess a short duration of action, with only 25% remaining in serum at 30 minutes post-injection in rhesus monkeys, making it an ideal agent for application in biomedical imaging, for instance in positron emission tomography (PET).Earlier analogues of LY-2459989 besides LY-2795050 with similar actions and potential uses have also been described.".
- LY-2459989 atcPrefix "None".
- LY-2459989 iupacName "3-Fluoro-4-[4-[[(2S)-2-pyridin-3-ylpyrrolidin-1-yl]methyl]phenoxy]benzamide".
- LY-2459989 thumbnail LY-2459989.svg?width=300.
- LY-2459989 wikiPageID "49155874".
- LY-2459989 wikiPageLength "4536".
- LY-2459989 wikiPageOutDegree "34".
- LY-2459989 wikiPageRevisionID "701855704".
- LY-2459989 wikiPageWikiLink Biological_imaging.
- LY-2459989 wikiPageWikiLink Buprenorphine.
- LY-2459989 wikiPageWikiLink CERC-501.
- LY-2459989 wikiPageWikiLink Carfentanil.
- LY-2459989 wikiPageWikiLink Category:Benzamides.
- LY-2459989 wikiPageWikiLink Category:Fluoroarenes.
- LY-2459989 wikiPageWikiLink Category:Kappa_antagonists.
- LY-2459989 wikiPageWikiLink Category:Opioid_antagonists.
- LY-2459989 wikiPageWikiLink Category:Pyridines.
- LY-2459989 wikiPageWikiLink Category:Pyrrolidines.
- LY-2459989 wikiPageWikiLink Category:Radiopharmaceuticals.
- LY-2459989 wikiPageWikiLink Category:Synthetic_opioids.
- LY-2459989 wikiPageWikiLink Central_nervous_system.
- LY-2459989 wikiPageWikiLink Diprenorphine.
- LY-2459989 wikiPageWikiLink Eli_Lilly.
- LY-2459989 wikiPageWikiLink Fluorine.
- LY-2459989 wikiPageWikiLink GR-89696.
- LY-2459989 wikiPageWikiLink Intravenous_therapy.
- LY-2459989 wikiPageWikiLink Isotopes_of_carbon.
- LY-2459989 wikiPageWikiLink LY-2795050.
- LY-2459989 wikiPageWikiLink Ligand_(biochemistry).
- LY-2459989 wikiPageWikiLink Naltrexone.
- LY-2459989 wikiPageWikiLink Naltriben.
- LY-2459989 wikiPageWikiLink Opioid_receptor.
- LY-2459989 wikiPageWikiLink Oral_administration.
- LY-2459989 wikiPageWikiLink Positron_emission_tomography.
- LY-2459989 wikiPageWikiLink Radioactive_tracer.
- LY-2459989 wikiPageWikiLink Receptor_(biochemistry).
- LY-2459989 wikiPageWikiLink Receptor_antagonist.
- LY-2459989 wikiPageWikiLink Rhesus_macaque.
- LY-2459989 wikiPageWikiLink Structural_analog.
- LY-2459989 wikiPageWikiLink Δ-opioid_receptor.
- LY-2459989 wikiPageWikiLink Κ-opioid_receptor.
- LY-2459989 wikiPageWikiLink Μ-opioid_receptor.
- LY-2459989 wikiPageWikiLinkText "LY-2459989".
- LY-2459989 atcPrefix "None".
- LY-2459989 c "23".
- LY-2459989 eliminationHalfLife "900.0".
- LY-2459989 f "1".
- LY-2459989 h "22".
- LY-2459989 iupacName "3".
- LY-2459989 molecularWeight "391.444".
- LY-2459989 n "3".
- LY-2459989 o "2".
- LY-2459989 routesOfAdministration Intravenous_therapy.
- LY-2459989 routesOfAdministration Oral_administration.
- LY-2459989 smiles "NCc1ccccc1".
- LY-2459989 stdinchi "InChI=1S/C23H22FN3O2/c24-20-13-177-10-2229-19-8-5-1615-27-12-2-4-2118-3-1-11-26-14-18/h1,3,5-11,13-14,21H,2,4,12,15H2,/t21-/m0/s1".
- LY-2459989 stdinchikey "DRGHCUTTXWIERB-NRFANRHFSA-N".
- LY-2459989 wikiPageUsesTemplate Template:Drugbox.
- LY-2459989 wikiPageUsesTemplate Template:Nervous-system-drug-stub.
- LY-2459989 wikiPageUsesTemplate Template:Opioidergics.
- LY-2459989 wikiPageUsesTemplate Template:Reflist.
- LY-2459989 subject Category:Benzamides.
- LY-2459989 subject Category:Fluoroarenes.
- LY-2459989 subject Category:Kappa_antagonists.
- LY-2459989 subject Category:Opioid_antagonists.
- LY-2459989 subject Category:Pyridines.
- LY-2459989 subject Category:Pyrrolidines.
- LY-2459989 subject Category:Radiopharmaceuticals.
- LY-2459989 subject Category:Synthetic_opioids.
- LY-2459989 hypernym Antagonist.
- LY-2459989 type ChemicalSubstance.
- LY-2459989 type Drug.
- LY-2459989 type ChemicalObject.
- LY-2459989 type Thing.
- LY-2459989 type Q8386.
- LY-2459989 comment "LY-2459989 is a silent antagonist of the κ-opioid receptor (KOR) that has been developed by Eli Lilly as a radiotracer (labeled with carbon-11) of the aforementioned receptor. It possesses high affinity for the KOR (Ki = 0.18 nM) and is highly selective for it over the μ-opioid receptor (Ki = 7.68 nM) and the δ-opioid receptor (Ki = 91.3 nM) (over 43-fold selectivity for the KOR over the other opioid receptors).".
- LY-2459989 label "LY-2459989".
- LY-2459989 sameAs Q22906626.
- LY-2459989 sameAs Q22906626.
- LY-2459989 wasDerivedFrom LY-2459989?oldid=701855704.
- LY-2459989 depiction LY-2459989.svg.
- LY-2459989 isPrimaryTopicOf LY-2459989.