LY2444296

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Chemical Structure| 1346133-11-6 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 :

无水乙醇: 25 mg/mL(61.21 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
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