Pitolisant hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Pitolisant HCl (BF2.649; Ciproxidine)是一种新型有效的和选择性的非咪唑反向激动剂,对重组人H3受体的Ki值为0.16 nM [1]。组胺H3受体是一种组胺自身受体,作为一种异源受体参与调节其他神经递质的释放,使其成为包括认知在内的许多适应症的有吸引力的药物靶标[2]。
体外实验:BF2.649为竞争性拮抗剂,Ki值为0.16 nM。BF2.649作为反向激动剂发挥作用,EC50值为1.5 nM,内在活性比ciproxifan高大约50%。Pitolisant对啮齿动物受体的体外效力约低6倍[1]。
在体实验:Pitolisant HCl是口服生物可利用的激动剂。在小鼠中,口服和静脉内给予pitolisant HCl时,曲线下血浆面积的比率为84%。BF2.649口服给药以剂量依赖性方式增强小鼠脑中的远-甲基组胺水平,其是代表组胺能神经元活性的指数,ED50值为1.6 mg/kg,重复给药后反应持续17天[1]。用20-、40-或60-mg剂量的pitolisant治疗,在9/14(64%)患者中具有统计学显著抑制效果(配对t-检验测定的标准化光敏反应[SPR]降低),其中6/14(43%)对间歇性光刺激(IPS)的反应消失[3]。在几种精神分裂症小鼠模型中,BF2.649表现出显著的抑制活性[4]。
参考文献:
Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, 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.
T A Esbenshade, K E Browman, R S Bitner, M Strakhova, M D Cowart, J D Brioni The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br J Pharmacol. 2008 Jul; 154(6): 1166–1181.
Kasteleijn-Nolst Trenité D, Parain D, Genton P, Masnou P, Schwartz JC, Hirsch E. Efficacy of the histamine 3 receptor (H3R) antagonist pitolisant (formerly known as tiprolisant; BF2.649) in epilepsy: dose-dependent effects in the human photosensitivity model. Epilepsy Behav.2013 Jul;28(1):66-70.
Ligneau X, Landais L, Perrin D, Piriou J, Uguen M, Denis E, Robert P, Parmentier R, Anaclet C, Lin JS, Burban A, Arrang JM,Schwartz JC. Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649. Biochem Pharmacol. 2007 Apr 15;73(8):1215-24. a
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 332.31 |
Cas No. | 903576-44-3 |
Formula | C17H27Cl2NO |
Synonyms | Ciproxidine;BF 2649;BF2649;BF-2649 |
Solubility | ≥16.6 mg/mL in DMSO; ≥57.4 mg/mL in H2O; ≥94.2 mg/mL in EtOH |
Chemical Name | 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine;hydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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