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Experimental drugs
LY-2459989
Другие языки:

    LY-2459989

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    LY-2459989
    LY-2459989.svg
    Clinical data
    Routes of
    administration    		 Oral, intravenous
    ATC code
    • None
    Pharmacokinetic data
    Elimination half-life 15 minutes (in rhesus monkeys)
    Identifiers
    • 3-Fluoro-4-[4-[[(2S)-2-pyridin-3-ylpyrrolidin-1-yl]methyl]phenoxy]benzamide
    CAS Number
    PubChem CID
    UNII
    Chemical and physical data
    Formula C23H22FN3O2
    Molar mass 391.446 g·mol−1
    3D model (JSmol)
    • NC(=O)c1ccc(Oc2ccc(CN3CCC[C@H]3c4cccnc4)cc2)c(F)c1
    • InChI=1S/C23H22FN3O2/c24-20-13-17(23(25)28)7-10-22(20)29-19-8-5-16(6-9-19)15-27-12-2-4-21(27)18-3-1-11-26-14-18/h1,3,5-11,13-14,21H,2,4,12,15H2,(H2,25,28)/t21-/m0/s1
    • Key:DRGHCUTTXWIERB-NRFANRHFSA-N

    LY-2459989 is a silent antagonist of the κ-opioid receptor (KOR) that has been developed by Eli Lilly as a radiotracer of the aforementioned receptor, labeled either with carbon-11 or fluorine-18. 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 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.

    See also



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