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Pitolisant HCl {[allProObj[0].p_purity_real_show]}

货号:A264451 同义名: BF 2649; Ciproxidine

Pitolisant HCl is an inverse agonist of human H3 receptor with Ki of 0.16 nM.

Pitolisant HCl 化学结构 CAS号:903576-44-3
Pitolisant HCl 化学结构
CAS号:903576-44-3
Pitolisant HCl 3D分子结构
CAS号:903576-44-3
Pitolisant HCl 化学结构 CAS号:903576-44-3
Pitolisant HCl 3D分子结构 CAS号:903576-44-3
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Pitolisant HCl 纯度/质量文件 产品仅供科研

货号:A264451 标准纯度: {[allProObj[0].p_purity_real_show]}
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Pitolisant HCl 生物活性

描述 The cerebral histaminergic neurons seem to play a critical role in the maintenance of wakefulness and higher cerebral functions, e.g., attention or learning. Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic neurons in brain and thereby promote vigilance and cognition. Pitolisant Hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor. Pitolisant behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM. In mice, the oral bioavailability coefficient, i.e., the ratio of plasma areas under the curve after oral and i.v. administrations, respectively, was 84%. Pitolisant dose dependently enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity, with an ED50 value of 1.6 mg/kg p.o., a response that persisted after repeated administrations for 17 days. In rats, the drug enhanced dopamine and acetylcholine levels in microdialysates of the prefrontal cortex. In cats, it markedly enhanced wakefulness at the expense of sleep states and also enhanced fast cortical rhythms of the electroencephalogram, known to be associated with improved vigilance[3].

Pitolisant HCl 参考文献

[1]McGaraughty S, Chu KL, et al. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009 Feb 18;158(4):1652-61.

[2]Ligneau X, Perrin D, 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.

[3]BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, Hydrochloride], a Nonimidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology

Pitolisant HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL

Pitolisant HCl 技术信息

CAS号903576-44-3
分子式C17H27Cl2NO
分子量 332.31
SMILES Code ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1.[H]Cl
MDL No. MFCD09970745
别名 BF 2649; Ciproxidine; Pitolisant; BF-2649 HCl; Tiprolisant hydrochloride; Pitolisant hydrochloride
运输蓝冰
InChI Key XLFKECRRMPOAQS-UHFFFAOYSA-N
Pubchem ID 11551689
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

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