Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dasotraline is a triple reuptake inhibitor that blocks dopamine(DA), norepinephrine(NE), and serotonin [5-hydroxytryptamine (5-HT)] transporters with IC 50 values of 4, 6, and 11 nM, respectively. Dasotraline represents a potential new class of antidepressant agents.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 2,140.00 | |
50 mg | 6-8 weeks | $ 2,785.00 | |
100 mg | 6-8 weeks | $ 3,520.00 |
Description | Dasotraline is a triple reuptake inhibitor that blocks dopamine(DA), norepinephrine(NE), and serotonin [5-hydroxytryptamine (5-HT)] transporters with IC 50 values of 4, 6, and 11 nM, respectively. Dasotraline represents a potential new class of antidepressant agents. |
In vivo | The present in-vivoelectrophysiological study is undertaken to determine the effects of the triple reuptake inhibitor Dasotraline (SEP-225289) on the neuronal activities of locus coeruleus (LC) NE, ventral tegmental area (VTA) DA and dorsal raphe (DR) 5-HT neurons. Administered acutely, Dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α 2, D 2 and 5-HT 1A 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. Dasotraline is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery (RT 50 ) of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. The recovery time (RT), from the suppression of hippocampus pyramidal neuron firing activity following microiontophoresis application of 5-HT and NE, is assessed by determining the RT 50 values before and after the acute intravenous administration of cumulative doses of Dasotraline (1–8 mg/kg). Although Dasotraline (1 and 2 mg/kg) does not modify the firing activity of CA3 pyramidal neurons, a significant reduction (~50%) is detected with the highest dose (8 mg/kg). In rats pre-treated with WAY100635, Dasotraline (0.5-2 mg/kg i.v.) elicits a significant increase in DR 5-HT firing rate. In rats pre-treated with WAY100635, Dasotralinesignificantly increases the number of single spikes and bursts [1]. |
Molecular Weight | 292.2 |
Formula | C16H15Cl2N |
CAS No. | 675126-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Dasotraline 675126-05-3 inhibitor inhibit