Cas No.: | 1346133-11-6 |
Synonyms: | LY2444296; FP3FBZ;LY-2444296;LY 2444296 |
SMILES: | O=C(C1C=C(F)C(OC2C=CC(CN3CCC[C@H]3C3C=C(F)C=CC=3)=CC=2)=CC=1)N |
Formula: | C24H22F2N2O2 |
M.Wt: | 408.440493106842 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. [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. |
Description: | 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]. |
Target: | Ki: ~1 nM (KOPR)[1] |
In Vivo: | LY2444296 displays anti-anxiety like effects in the EPM test[1]. LY2444296 (3 mg/kg; i.p.; 30 min before U69,593 administration) prevents behavioral and neuroendocrine effects caused by the reference kappa agonist U69,593 in cocaine-naïve rats[2]. LY2444296 reduces anxiety-like and depressive-like behaviors, as well as CORT release, in rats tested after chronic extended access cocaine self-administration, but not in cocaine-naïve rats[2]. Animal Model: Adult male Sprague Dawley rats (240–250 g)[2] Dosage: 3 mg/kg Administration: Injected intraperitoneally; 30 min before U69,593 administration Result: Prevented behavioral and neuroendocrine effects caused by U69,593 in cocaine-naïve rats. |
References: | [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. [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 |