1. Neuronal Signaling
  2. Dopamine Transporter
    Serotonin Transporter

Dasotraline (Synonyms: SEP 225289)

Cat. No.: HY-12850
Handling Instructions

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

For research use only. We do not sell to patients.

Dasotraline Chemical Structure

Dasotraline Chemical Structure

CAS No. : 675126-05-3

Size Price Stock
1 mg USD 110 Get quote
5 mg USD 370 Get quote
10 mg USD 660 Get quote
25 mg USD 1250 Get quote
50 mg USD 2200 Get quote

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  • Biological Activity

  • Technical Information

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  • References

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (106.09 mM)

*"≥" 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
10 mM 0.3422 mL 1.7112 mL 3.4223 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

292.20

Formula

C₁₆H₁₅Cl₂N

CAS No.

675126-05-3

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Dasotraline
Cat. No.:
HY-12850
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Dasotraline

Cat. No.: HY-12850