| Name | Dasotraline hydrochloride |
| Description | Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that inhibits dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. |
| In vivo | Acute administration of dasotraline decreases the spontaneous firing rate of LC NE (norepinephrine), VTA DA (dopamine), and DR 5-HT (serotonin) neurons in a dose-dependent manner by activating α2, D2, and 5-HT1A autoreceptors, respectively. Primarily, dasotraline significantly reduces the firing rate of LC NE neurons, while moderately impacting VTA DA and DR 5-HT neuronal activity. Concurrently, SEP-225289, known as (dasotraline), demonstrates equal potency in inhibiting both 5-HT and NE transporters, effectively extending the time for a 50% recuperation of firing activity in dorsal hippocampus CA3 pyramidal neurons following the inhibition induced by the microiontophoretic application of 5-HT and NE. Moreover, the average occupancies of dopamine and serotonin transporters by SEP-225289 escalate with dose increments, showing transporter occupancies of approximately 33%±11% and 2%±13% for 8 mg, 44%±4% and 9%±10% for 12 mg, and 49%±7% and 14%±15% for 16 mg, for dopamine and serotonin transporters, respectively. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 31 mg/mL (94.32 mM)
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| Keywords | Dasotraline | Dopamine Transporter | inhibit | Dasotraline hydrochloride | Dasotraline Hydrochloride | Inhibitor | SERT | SEP-225289 | SEP 225289 Hydrochloride | SEP225289 Hydrochloride | SLC6A4 | SEP 225289 | 5-HTT | DAT | Serotonin Transporter | SEP225289 | SLC6A3 | SEP-225289 Hydrochloride |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Octopamine hydrochloride | Oxolinic acid | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
