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 |