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362665-57-4

中文名稱 PITOLISANT 草酸鹽
英文名稱 Tiprolisant oxalate
CAS 362665-57-4
分子式 C19H28ClNO5
分子量 385.882
MOL 文件 362665-57-4.mol
362665-57-4 結(jié)構(gòu)式 362665-57-4 結(jié)構(gòu)式

基本信息

中文別名
替洛利生草酸鹽
PITOLISANT 草酸鹽
英文別名
Tiprolisant oxalate
Pitolisant (oxalate)
Pitolisant ethanedioate (1:1)
1-[3-[3-(4-Chlorophenyl)propoxy]propyl]piperidine ethanedioate (1:1)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : 50 mg/mL (129.57 mM; Need ultrasonic)
形態(tài)粉末
顏色Off-white to light yellow

常見問題列表

生物活性
Pitolisant oxalate 是一種有效的選擇性人重組 H3 受體選擇性反向激動劑,Ki 為 0.16 nM。
靶點

Ki: 0.16 nM (H3 receptor)
EC50: 1.5 nM (H3 receptor)

體外研究

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.

體內(nèi)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.

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