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| Routes of administration | Oral,intravenous |
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| Pharmacokinetic data | |
| Eliminationhalf-life | 15 minutes (in rhesus monkeys)[1] |
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| Chemical and physical data | |
| Formula | C23H22FN3O2 |
| Molar mass | 391.446 g·mol−1 |
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LY-2459989 is asilent antagonist of theκ-opioid receptor (KOR) that has been developed byEli Lilly as aradiotracer of thatreceptor, labeled either withcarbon-11[1] orfluorine-18.[2] It possesses highaffinity for the KOR (Ki = 0.18 nM) and is highly selective for it over theμ-opioid receptor (Ki = 7.68 nM) and theδ-opioid receptor (Ki = 91.3 nM) (over 43-fold selectivity for the KOR over the otheropioid receptors).[1] LY-2459989 is afluorine-containinganalogue and follow-up compound ofLY-2795050, the first KOR-selective antagonist radiotracer.[1] Relative to LY-2795050, LY-2459989 displays 4-fold higher affinity for the KOR and similar selectivity and also possesses greatly improvedcentral nervous system permeation (brain levels were found to be 6-fold higher than those of LY-2795050).[1] The drug appears to possess a short duration of action, with only 25% remaining in serum at 30 minutes post-injection inrhesus monkeys, making it an ideal agent for application inbiomedical imaging, for instance inpositron emission tomography (PET).[1]
Earlier analogues of LY-2459989 besides LY-2795050 with similar actions and potential uses have also been described.[3]
