1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDasotralineCat. No.: HY-12850CAS No.: 675126-05-3Synonyms: SEP 225289分式: CHClN分量: 292.2作靶點: Dopamine Transporter; Serotonin Transporter作通路: Neuronal Signaling儲存式: Please store the product under the recommended conditions inthe C

2、OA.溶解性數(shù)據(jù)體外實驗 DMSO : 31 mg/mL (106.09 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4223 mL 17.1116 mL 34.2231 mL5 mM 0.6845 mL 3.4223 mL 6.8446 mL10 mM 0.3422 mL 1.7112 mL 3.4223 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Da

3、sotraline種三重 再攝取抑制劑，阻斷多巴胺 (dopamine)，去甲腎上腺素 (norepinephrine) 和 5-羥胺(5-HT) 轉(zhuǎn)運蛋，IC50 值分別為 4, 6 和 11 nM。IC50 & Target IC50: 4 nM (dopamine transporter), 6 nM (norepinephrine transporter),11 nM (5-HT transporter) 1體內(nèi)研究The present in-vivoelectrophysiological study is undertaken to determine the effects o

4、f the triple reuptakeinhibitor Dasotraline (SEP-225289) on the neuronal activities of locus coeruleus (LC) NE, ventral tegmental1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEarea (VTA) DA and dorsal raphe (DR) 5-HT neurons. Administered acutely, Dasotraline dose-dependentlydecreases the spontaneo

5、us firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of 2,D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NEneurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. Dasotraline isequipotent at

6、inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a50% recovery (RT50) of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibitioninduced by microiontophoretic application of 5-HT and NE. The recovery time (RT), from the suppres

7、sion ofhippocampus pyramidal neuron firing activity following microiontophoresis application of 5-HT and NE, isassessed by determining the RT50 values before and after the acute intravenous administration ofcumulative doses of Dasotraline (18 mg/kg). Although Dasotraline (1 and 2 mg/kg) does not mod

8、ify thefiring activity of CA3 pyramidal neurons, a significant reduction (-50%) is detected with the highest dose (8mg/kg). In rats pre-treated with WAY100635, Dasotraline (0.5-2 mg/kg i.v.) elicits a significant increase in DR5-HT firing rate. In rats pre-treated with WAY100635, Dasotralinesignific

9、antly increases the number of singlespikes and bursts 1.REFERENCES1. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int JNeuropsychopharmacol. 2011 Mar;14(2):211-23.McePdfHeightCaution: Product has not been fully validated for medical