同义名 :	FP3FBZ
	CAS号 :	1346133-11-6
	货号 :	A724727
	分子式 :	C24H22F2N2O2
	纯度 :	99%+
	分子量 :	408.44
	MDL号 :	MFCD32067413
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. 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. 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[3]. LY2444296 [subcutaneous (s.c.) injection] at 10 and 30mg/kg, but not 3mg/kg, significantly decreased immobility time in a dose-dependent manner. LY2444296 and ADL5859 yielded significant synergistic effects for the antidepressant-like effect at the combined dose ranging from 3.84 mg/kg to 9.0 mg/kg[4]. κ(kappa)-selective doses of both LY2444296 (0.032-1 mg/kg) and LY2795050 (0.032-0.32 mg/kg) dose- and time-dependently prevented the grooming deficits caused by salvinorin A (1.8 m/kg)[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.45mL 0.49mL 0.24mL	12.24mL 2.45mL 1.22mL	24.48mL 4.90mL 2.45mL

参考文献

[1]Huang P, Tunis J, et al. Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. Eur J Pharmacol. 2016 Jun 15;781:53-9. [2]Huang P, Yakovleva T, 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. [3]Valenza M, Butelman ER, Kreek MJ. "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 [4]Huang P, Tunis J, Parry C, Tallarida R, Liu-Chen LY. Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. Eur J Pharmacol. 2016 Jun 15;781:53-9 [5]Butelman ER, McElroy BD, Prisinzano TE, Kreek MJ. Impact of Pharmacological Manipulation of the κ-Opioid Receptor System on Self-grooming and Anhedonic-like Behaviors in Male Mice. J Pharmacol Exp Ther. 2019 Jul;370(1):1-8