S87162-10mg Pitolisant HCl 903576-44-3 99% 10mg 840.00 现货

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商品详情

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产品描述： Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
靶点： Ki: 0.16 nM (H3 receptor) EC50: 1.5 nM (H3 receptor)
体内研究： The administration of Pitolisantat a single dose of 10 mg/kg 30 min before a single dose of LY170053 (2 mg/kg b.w.) also significantly affects immobility time in the FST. Subsequent administration of the aforementioned drug sequence in mice statistically significantly increases the duration of immobility in comparison to the time determined in the control group in the FST. It decreased locomotor activity as well. In contrast, the results obtained in subchronic treatment after fifteen administrations of both drugs (Pitolisant 10 mg/kg b.w., and after 30 min LY170053 2 mg/kg b.w., and again after 4 h LY170053 2 mg/kg b.w.) show that the administration of Pitolisant followed by that of LY170053 equalized the locomotor activity in mice; in comparison to the level of motility in the control group, to which only Pitolisant is administered. More importantly, this combination of drugs significantly reduces immobility time to the level obtained in the control group in the forced swim test in mice [one-way ANOVA; F(3,20)=4.226,P=0.0181]. Rats given Pitolisant (10 mg/kg) during the conditioning phase stayed 502±94 s on the paired texture, a value not statistically different from that of controls, indicating that Pitolisant did not support place preference
参考文献：
1. Ligneau X, et al. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J Pharmacol Exp Ther. 2007 Jan;320(1):365-75. 2. Dudek M, et al. H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by LY170053 in mice. Metab Brain Dis. 2016 Oct;31(5):1023-9. 3. Uguen M, et al. Preclinical evaluation of the abuse potential of Pitolisant, a histamine H? receptor inverse agonist/antagonist compared with CRL 40476. Br J Pharmacol. 2013 Jun;169(3):632-44.
溶解性： Soluble in DMSO、H2O
保存条件： RT
配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.012 ml	15.06 ml	30.12 ml
5 mM	0.602 ml	3.012 ml	6.024 ml
10 mM	0.301 ml	1.506 ml	3.012 ml
50 mM	0.06 ml	0.301 ml	0.602 ml

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