Dasotraline hydrochloride |
Katalog-Nr.GC19118 |
Dasotralin-Hydrochlorid (SEP-225289-Hydrochlorid) ist ein dreifacher Wiederaufnahmehemmer, der Dopamin-, Norepinephrin- und Serotonin-Transporter mit IC50-Werten von 4, 6 bzw. 11 nM blockiert.
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Cas No.: 675126-08-6
Sample solution is provided at 25 µL, 10mM.
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
Acute administration of 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. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE[1]. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg[2].
References:
[1]. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int J Neuropsychopharmacol. 2011 Mar;14(2):211-23.
[2]. DeLorenzo C, et al. SEP-225289 serotonin and dopamine transporter occupancy: a PET study.
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