產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg
CAS	903576-44-3
別名	Ciproxidine;BF 2649;BF2649;BF-2649
化學(xué)名	1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine;hydrochloride
分子式	C17H27Cl2NO
分子量	332.31
溶解度	≥ 16.6 mg/mL in DMSO, ≥ 94.2 mg/mL in EtOH, ≥ 57.4 mg/mL in H2O
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Pitolisant HCl (BF2.649; Ciproxidine) is a potent, novel, and selective nonimidazole inverse agonist at the recombinant human H3 receptor with a Ki value of 0.16 nM[1]. The histamine H3 receptor, a histamine autoreceptor, functions as a heteroreceptor that regulates the release of other neurotransmitters, making it an attractive drug target for a number of indications including cognition [2].

In vitro: BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM. BF2.649 functioned as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity about 50% higher than that of ciproxifan. Pitolisant in vitro potency was approximately 6 times lower at the rodent receptor [1].

In vivo: Pitolisant HCl was an oral bioavailable agonist. In mice, after oral and i.v. administrations of pitolisant HCl, the ratio of plasma areas under the curve was 84%. BF2.649 enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity in a dose dependent manner with an ED50 value of 1.6 mg/kg p.o. The response persisted after repeated administrations for 17 days [1]. Treatment with 20-, 40-, or 60-mg doses of pitolisant showed a statistically significant suppressive effect (standardized photosensitive response [SPR] reduction as measured with paired t-tests) in 9/14 (64%) patients of whom 6/14 (43%) showed abolition of the response to intermittent photic stimulation (IPS) [3]. BF2.649 showed significant inhibitory activity in several mouse models of schizophrenia [4].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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