1346133-11-6

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ～1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].

LY2444296 is a brain-penetrantorally activeshort-actinghigh-affinitypotent and selective K (kappa) opioid receptor (KOR) antagonist (human K/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/K21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses K agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by r at formalin test)decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming.

κ Opioid Receptor/KOR

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[1] Huang P, et al. Two short-acting kappa opioid receptor antagonists (zyklophin and LY2444296) exhibited different behavioral effects from the long-acting antagonist norbinaltorphimine in mouse anxiety tests. Neurosci Lett. 2016 Feb 26;615:15-20. DOI:10.1016/j.neulet.2016.01.017
[2] Valenza M, et al. "Effects of the novel relatively short-acting kappa opioid receptor antagonist LY2444296 in behaviors observed after chronic extended-access cocaine self-administration in rats". Psychopharmacology (Berl). 2017 Aug;234(15):2219-2231. DOI:10.1007/s00213-017-4647-0