Cas No.: | 675126-08-6 |
Chemical Name: | Dasotraline hydrochloride |
Synonyms: | (1R,4S)-N-Desmethyl Sertraline Hydrochloride;(1R,4S)-4-(3,4;(1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine Hydrochlorid;(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine Hydrochloride;(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-ylamine hydrochloride;(1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine hydrochloride;(1R,4S)-trans-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine HCl;NorSertraline;SEP 225289 hydrochloride;SEP-225289 hydrochloride;Dasotraline hydrochloride;Dasotraline HCl;1VIY7J4C0I;Dasotraline hydrochloride [USAN];Dasotraline (hydrochloride);Dasotraline hydrochloride (USAN);Dastroline;rac-trans-N-Desmethyl Sertraline Hydrochloride;(1R,4S)-trans-Norsertraline hydrochloride;Norsertraline hydrochloride, (1R,4S)-trans- |
SMILES: | ClC1=C(C([H])=C([H])C(=C1[H])[C@@]1([H])C2=C([H])C([H])=C([H])C([H])=C2[C@@]([H])(C([H])([H])C1([H])[H])N([H])[H])Cl.Cl[H] |
Formula: | C16H16Cl3N |
M.Wt: | 328.6639 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |
In Vivo: | 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]. |