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 | This in-vivo electrophysiological study investigates the impact of Dasotraline (SEP-225289), a triple reuptake inhibitor, on the firing activities of locus coeruleus (LC) NE, ventral tegmental area (VTA) DA, and dorsal raphe (DR) 5-HT neurons. Administered acutely, Dasotraline effectively reduces the spontaneous firing rates of these neurons in a dose-dependent manner, primarily through the activation of α2, D2, and 5-HT1A autoreceptors for LC NE, VTA DA, and DR 5-HT neurons, respectively. While Dasotraline notably suppresses LC NE neuronal activity, it only partially reduces VTA DA and DR 5-HT neuron firing rates. The compound shows equal potency in inhibiting 5-HT and NE transporters, extending the recovery time (RT50) for dorsal hippocampus CA3 pyramidal neurons’ firing activity post-inhibition from microiontophoretic applications of 5-HT and NE. Although lower doses of Dasotraline (1 and 2 mg/kg) do not affect CA3 pyramidal neurons' firing activity, a 50% reduction is observed with the highest dose (8 mg/kg). Additionally, when rats are pre-treated with WAY100635, Dasotraline administration (0.5-2 mg/kg i.v.) significantly boosts the firing rate of DR 5-HT neurons, as well as the quantity of single spikes and bursts. |
Molecular Weight | 292.2 |
Formula | C16H15Cl2N |
CAS No. | 675126-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Dasotraline 675126-05-3 inhibitor inhibit