Pitolisant - CAS:362665-56-3

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Pitolisant (Synonyms:Tiprolisant)

目录号 : KM2850 CAS No. : 362665-56-3 纯度 : 97%

Data Sheet 产品使用指南

Pitolisant 是一种有效的选择性的非咪唑类重组人组胺 H3 受体反相激动剂，K_i 为 0.16 nM。

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生物活性

Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

体外研究

On the stimulation of guanosine 5′-O-(3-[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 EC₅₀ value of 1.5 nM and an intrinsic activity ~50% higher than that of ciproxifan. Pitolisant displaces [I]iodoproxyfan binding from mouse brain cortical membranes with an IC₅₀ 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 [I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H₃ receptor with an IC₅₀ 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 IC₅₀ 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 [S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC₅₀ value of 1.5±0.1 nM.

体内研究

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]. 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.

分子式

C₁₇H₂₆ClNO

分子量

295.85

CAS号

362665-56-3

中文名称

替洛利生

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (338.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3801 mL	16.9005 mL	33.8009 mL
5 mM	0.6760 mL	3.3801 mL	6.7602 mL
10 mM	0.3380 mL	1.6900 mL	3.3801 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.45 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.45 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.45 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。