|1-(3-(3-(4-氯苯基)丙氧基)丙基)哌啶盐酸盐|CsnPharm

CAS No.: 903576-44-3

Pitolisant HCl/BF 2649 盐酸盐 Catalog No. CSN18554

Synonyms: Ciproxidine;BF 2649;BF 2649 HCl

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

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Histamine Receptor H3

Ki:0.16nM
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 K_i 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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03152123	Healthy Drug ... more >>Abuse Collapse <<	Phase 1	Completed	-	Canada, Ontario ... more >> INC Research Toronto, Ontario, Canada, M5V 2T3 Collapse <<

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0093 mL
- 15.0463 mL
- 30.0925 mL
- 5 mM
- 0.6019 mL
- 3.0093 mL
- 6.0185 mL
- 10 mM
- 0.3009 mL
- 1.5046 mL
- 3.0093 mL

技术信息

CAS号

903576-44-3

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H27Cl2NO

运输

蓝冰

分子量

332.31

别名

Ciproxidine;BF 2649;BF 2649 HCl;FUB-649;HBS-101;Tiprolisant;Pitolisant HCl

溶解度

DMSO	66.0 mg/mL (198.6 mM)
Ethanol	66.0 mg/mL (198.6 mM)

动物实验配方

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Pitolisant HCl/BF 2649 盐酸盐 Catalog No. CSN18554

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