Dasotraline hydrochloride|675126-08-6|(SEP-225289 hydrochloride)-陌孚医药/Medlife

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Dasotraline hydrochloride (Synonyms: SEP-225289 hydrochloride)

目录号: PL11259 纯度: ≥99%

CAS No. :675126-08-6

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中文名称	Dasotraline hydrochloride
中文别名	(1R,4S)-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺盐酸盐(1:1);达索曲林盐酸盐;氯化钪（III）水合物
英文名称	Dasotraline hydrochloride
英文别名	(1R,4S)-N-Desmethyl Sertraline Hydrochloride;(1R,4S)-4-(3,4;(1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine Hydrochlorid;(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine Hydrochloride;(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-ylamine hydrochloride;(1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine hydrochloride;(1R,4S)-trans-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine HCl;NorSertraline;SEP 225289 hydrochloride;SEP-225289 hydrochloride;Dasotraline hydrochloride;Dasotraline HCl;1VIY7J4C0I;Dasotraline hydrochloride [USAN];Dasotraline (hydrochloride);Dasotraline hydrochloride (USAN);Dastroline;rac-trans-N-Desmethyl Sertraline Hydrochloride;(1R,4S)-trans-Norsertraline hydrochloride;Norsertraline hydrochloride, (1R,4S)-trans-
Cas No.	675126-08-6
分子式	C₁₆H₁₆Cl₃N
分子量	328.66
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Dasotraline hydrochloride (SEP-225289 hydrochloride) 是具有阻断多巴胺，去甲肾上腺素和三羟色胺转运蛋白的三重再摄取抑制剂，IC₅₀值分别为4，6和11 nM。

生物活性

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC 50 values of 4, 6, and 11 nM, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 4 nM (dopamine), 6 nM (norepinephrine), 11 nM (serotonin)

体内研究(In Vivo)

Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7%

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int J Neuropsychopharmacol. 2011 Mar;14(2):211-23.
[2]. DeLorenzo C, et al. SEP-225289 serotonin and dopamine transporter occupancy: a PET study.

溶解度数据	In Vitro: DMSO : ≥ 31 mg/mL (94.32 mM)H₂O : 1.61 mg/mL (4.90 mM; ultrasonic and warming and heat to 60°C)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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