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Pitolisant

产品编号 T60636 CAS 362665-56-3

Pitolisant 是一种有效的选择性的非咪唑类反相激动剂，作用于重组人组胺H3受体反相激动剂，Ki 值为 0.16 nM。

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Pitolisant, CAS 362665-56-3

规格	价格/CNY		货期	数量
2 mg	￥ 294		现货

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其他形式的 Pitolisant:

Pitolisant hydrochloride
现货
Pitolisant oxalate
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生物活性

化学信息

存储 & 溶解度

产品描述	Pitolisant is a potent and selective nonimidazole inverse agonist that acts on the recombinant human histamine H3 receptor with Ki of 0.16 nM.
体外活性	On the stimulation of guanosine 5′-O-(3-[ 35 S]thio)triphosphate binding to this receptor, Pitolisant (BF2.649) behaves as a competitive antagonist with a K i value of 0.16 nM and as an inverse agonist with an EC 50 value of 1.5 nM and an intrinsic activity ~50% higher than that of ciproxifan. Pitolisant displaces [ 125 I]iodoproxyfan binding from mouse brain cortical membranes with an IC 50 value of 26.4±4.5 nM. Taking into account the K d value of the radioligand (161±9 pM), the deduced K i value for Pitolisant is 14±1 nM. Pitolisant displaces [ 125 I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H 3 receptor with an IC 50 value of 4.2±0.2 nM. Taking into account the K d value of the radioligand (50±4 pM), the deduced K i value for Pitolisant is 2.7±0.5 nM. Pitolisant progressively reverses this response with a Hill coefficient close to unity and an IC 50 value of 330±68 nM, leading to a K i value of 17±4 nM. Pitolisant elicits a dose-dependent decrease of the basal-specific [ 35 S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC 50 value of 1.5±0.1 nM [1].
体内活性	The administration of Pitolisantat a single dose of 10 mg/kg 30 min before a single dose of Olanzapine (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 Olanzapine 2 mg/kg b.w., and again after 4 h Olanzapine 2 mg/kg b.w.) show that the administration of Pitolisant followed by that of Olanzapine 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] [2]. 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 [3].

分子量	295.85
分子式	C17H26ClNO
CAS No.	362665-56-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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