PITOLISANT 草酸盐
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- CAS号:
- 362665-57-4
- 英文名:
- Tiprolisant oxalate
- 英文别名:
- Tiprolisant oxalate;Pitolisant (oxalate);Pitolisant ethanedioate (1:1);1-[3-[3-(4-Chlorophenyl)propoxy]propyl]piperidine ethanedioate (1:1)
- 中文名:
- PITOLISANT 草酸盐
- 中文别名:
- 替洛利生草酸盐;化合物 T12491;PITOLISANT 草酸盐
- CBNumber:
- CB02666675
- 分子式:
- C19H28ClNO5
- 分子量:
- 385.88232
- MOL File:
- 362665-57-4.mol
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PITOLISANT 草酸盐化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : 50 mg/mL (129.57 mM; Need ultrasonic)
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形态:
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Powder
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颜色:
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Off-white to light yellow
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PITOLISANT 草酸盐性质、用途与生产工艺
Pitolisant oxalate 是一种有效的选择性人重组 H3 受体选择性反向激动剂,Ki 为 0.16 nM。
Ki: 0.16 nM (H3 receptor)
EC50: 1.5 nM (H3 receptor)
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.
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.
PITOLISANT 草酸盐
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362665-57-4, PITOLISANT 草酸盐 相关搜索:
- C17H26ClNOC2H2O4
- 化合物 T12491
- 替洛利生草酸盐
- PITOLISANT 草酸盐
- 362665-57-4
- Pitolisant ethanedioate (1:1)
- 1-[3-[3-(4-Chlorophenyl)propoxy]propyl]piperidine ethanedioate (1:1)
- Tiprolisant oxalate
- Pitolisant (oxalate)