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替洛利生盐酸盐  ≥98%

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包装规格：100mg in glass bottle
溶解性：溶于H2O（100mg/mL超声）和 DMSO（≥43mg/mL）
产品描述：基本信息 产品编号： P11144  产品名称： Pitolisant hydrochloride CAS: 903576-44-3   储存条件 粉末 -20℃ 四年     分子式： C17H26ClNO.HCl 溶于液体 -80℃ 6个月 分子量： 332.31 -20℃ 1个月 化学名：  1-(3-(3-(4-Chlorophenyl)propoxy)propyl)piperidine hydrochloride Solubility (25°C)：   体外:   DMSO 66mg/mL (198.6mM) Ethanol 66mg/mL (198.6mM) Water 66mg/mL (198.6mM) 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.0092mL 15.0462mL 30.0924mL 5mM 0.6018mL 3.0092mL 6.0185mL 10mM 0.3009mL 1.5046mL 3.0092mL 50mM 0.0602mL 0.3009mL 0.6018mL   生物活性 产品描述 一种新型的人重组H3受体选择性反向激动剂，Ki为0.16nM。 靶点 Ki:0.16nM (H3 receptor)EC50:1.5nM (H3 receptor)   体外研究 On the stimulation of guanosine 5′-O-(3-[35S]thio)triphosphate binding to this receptor,Pitolisant (BF2.649) behaves as a competitive antagonist with a Ki value of 0.16nM and as an inverse agonist with an EC50 value of 1.5nM and an intrinsic activity ~50% higher than that of ciproxifan.Pitolisant displaces [125I]iodoproxyfan binding from mouse brain cortical membranes with an IC50 value of 26.4±4.5nM.Taking into account the Kd value of the radioligand (161±9 pM),the deduced Ki value for Pitolisant is 14±1nM.Pitolisant displaces [125I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H3 receptor with an IC50 value of 4.2±0.2nM.Taking into account the Kd value of the radioligand (50±4 pM),the deduced Ki value for Pitolisant is 2.7±0.5nM.Pitolisant progressively reverses this response with a Hill coefficient close to unity and an IC50 value of 330±68nM,leading to a Ki value of 17±4nM.Pitolisant elicits a dose-dependent decrease of the basal-specific [35S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC50 value of 1.5±0.1nM. 体内研究 The administration of Pitolisantat a single dose of 10mg/kg 30 min before a single dose of LY170053 (2mg/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 10mg/kg b.w.,and after 30 min LY170053 2mg/kg b.w.,and again after 4h LY170053 2mg/kg b.w.) show that the administration of Pitolisant followed by that of LY170053 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 (10mg/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.   推荐实验方法(仅供参考) 激酶实验： [35S]GTPγS binding assays are performed.CHO-K1 cells stably expressing the human H3 receptor (~400 fmol/mg protein) are homogenized in ice-cold buffer (50mM Tris/HCl,pH 7.4).Homogenates are centrifuged twice (20,000g for 10 min at 4℃),and the final pellet is resuspended in 50 volumes of buffer. Membranes (550μg of protein) are pretreated with adenosine deaminase (1 U/mL) and incubated for 60 min at 25℃ with 0.1nM [35S]GTPγS and the drugs to be tested in a final volume of 1mL of assay buffer (50mM Tris/HCl,50mM NaCl,5mM MgCl2,10μM GDP,and 0.02% bovine serum albumin,pH 7.4).The nonspecific binding is determined using 10μM nonradioactive GTPγS.Incubations are stopped by rapid filtration under vacuum through GF/B glass fiber filters.After washing with ice-cold water,the radioactivity trapped on filters is counted by liquid scintillation spectrometry.A similar assay is used to assess competitive antagonism.In brief,membranes (10μg of protein) of HEK-293 cells stably expressing the human H3 receptor (~600 fmol/mg protein) are preincubated in presence of Pitolisant in the buffer (50mM Tris/HCl,pH 7.4,10mM MgCl2,100mM NaCl, and 10μM GDP) in a 96-well microplate under gentle agitation at room temperature (19-20℃) for 30 min before the addition of 0.1nM [35S]GTPγS (final volume 200μL).The nonspecific binding is determined using a 10μM concentration of nonradioactive GTPγS.After 30 min,incubations performed in triplicate are stopped by rapid filtration under vacuum on a Multiscreen MAFCOB50 microplate.Radioactivity trapped on filters is counted by liquid scintillation spectrometry.   动物实验:   Rats Male Wistar rats (220-300g) receive vehicle (methylcellulose 1%,p.o.),and Pitolisant (10mg/kg,p.o.).Ninety minutes later,they are killed by decapitation and nucleus accumbens are dissected out,weighed,frozen in liquid nitrogen and stored at-80℃.Tissues are homogenized in 1mL of a 0.4 N perchloric acid/2.7mM EDTA solution.After centrifugation (8000 rpm,20 min,4℃),supernatants are analysed by HPLC coupled to electrochemical detection.
保存条件：-20℃

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