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PITOLISANT HCL
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PITOLISANT HCL图片
CAS NO:903576-44-3
规格:≥98%
包装与价格:
包装价格(元)
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产品介绍
Pitolisant HCl (formerly also known as BF2.649; BF2649; Ciproxidine; Wakix) is a nonimidazole-based inverse agonist of the recombinant human histamine H3 receptor approved in 2019 for the treatment of excessive daytime sleepiness in adults with narcolepsy. It activates H3 receptor with Ki of 0.16 nM. Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic neurons in brain and thereby promote vigilance and cognition. On the stimulation of guanosine 5'-O-(3-[35S]thio)triphosphate binding to this receptor, BF2.649 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 and an intrinsic activity approximately 50% higher than that of ciproxifan. Its in vitro potency was approximately 6 times lower at the rodent receptor. 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%. BF2.649 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. On the two-trial object recognition test in mice, a promnesiant effect was shown regarding either scopolamine-induced or natural forgetting. These preclinical data suggest that BF2.649 is a valuable drug candidate to be developed in wakefulness or memory deficits and other cognitive disorders.
理化性质和储存条件


Name: Pitolisant HCl
CAS#: 903576-44-3 (HCl)
Chemical Formula: C17H27Cl2NO
Exact Mass: 295.1703
Molecular Weight: 332.309
Elemental Analysis: C, 61.44; H, 8.19; Cl, 21.34; N, 4.22; O, 4.81
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationFUB-649, BF-2649; B F2649; FUB649, BF2649; FUB 649; BF2.649; Pitolisant, Tiprolisant; Pitolisant HCl; Pitolisant hydrochloride
Chemical Name: 1-(3-(3-(4-Chlorophenyl)propoxy)propyl)piperidine hydrochloride
InChi Key: XLFKECRRMPOAQS-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H26ClNO.ClH/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19;/h7-10H,1-6,11-15H2;1H
SMILES Code: ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1.[H]Cl