13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
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化學性質：
| 規格 | 10mM (in 1mL DMSO) 10mg 50mg |
| CAS | 903576-44-3 |
| 別名 | Ciproxidine;BF 2649;BF2649;BF-2649 |
| 化學名 | 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 |
產品描述：
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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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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