2. Neuronal Signaling
  3. Dopamine Transporter Serotonin Transporter
  4. Dasotraline

Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Dasotraline hydrochloride) usually boasts enhanced water solubility and stability.

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Dasotraline Chemical Structure

Dasotraline Chemical Structure

CAS No. : 675126-05-3

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Dasotraline Related Antibodies

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Description

Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

IC50 & Target

IC50: 4 nM (dopamine transporter), 6 nM (norepinephrine transporter),11 nM (5-HT transporter)[1]
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 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. Dasotraline is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery (RT50) 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 RT50 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

292.20

Formula

C16H15Cl2N
CAS No.
SMILES

N[C@@H]1CC[C@@H](C2=CC=C(Cl)C(Cl)=C2)C3=CC=CC=C31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (106.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4223 mL 17.1116 mL 34.2231 mL
5 mM 0.6845 mL 3.4223 mL 6.8446 mL
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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4223 mL 17.1116 mL 34.2231 mL 85.5578 mL
5 mM 0.6845 mL 3.4223 mL 6.8446 mL 17.1116 mL
10 mM 0.3422 mL 1.7112 mL 3.4223 mL 8.5558 mL
15 mM 0.2282 mL 1.1408 mL 2.2815 mL 5.7039 mL
20 mM 0.1711 mL 0.8556 mL 1.7112 mL 4.2779 mL
25 mM 0.1369 mL 0.6845 mL 1.3689 mL 3.4223 mL
30 mM 0.1141 mL 0.5704 mL 1.1408 mL 2.8519 mL
40 mM 0.0856 mL 0.4278 mL 0.8556 mL 2.1389 mL
50 mM 0.0684 mL 0.3422 mL 0.6845 mL 1.7112 mL
60 mM 0.0570 mL 0.2852 mL 0.5704 mL 1.4260 mL
80 mM 0.0428 mL 0.2139 mL 0.4278 mL 1.0695 mL
100 mM 0.0342 mL 0.1711 mL 0.3422 mL 0.8556 mL
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Dasotraline Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dasotraline675126-05-3SEP 225289SEP225289SEP-225289Dopamine TransporterSerotonin TransporterDATSLC6A35-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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