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Dasotraline (hydrochloride)

Names

[ CAS No. ]:
675126-08-6

[ Name ]:
Dasotraline (hydrochloride)

[Synonym ]:
(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-ylamine hydrochloride
UNII:1VIY7J4C0I
(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine Hydrochloride
SEP-225289 HCI
(1R,4S)-trans-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine HCl
trans-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine hydrochloride
(1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine hydrochloride (1:1)
NorSertraline
(1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine hydrochloride
(1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine Hydrochlorid
1-Naphthalenamine, 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-, (1R,4S)-, hydrochloride (1:1)
(1R,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine Hydrochloride
(1R,4S)-N-Desmethyl Sertraline Hydrochloride
Dasotraline (hydrochloride)

Biological Activity

[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.

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter
Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter
Research Areas >> Neurological Disease

[Target]

IC50: 4 nM (dopamine), 6 nM (norepinephrine), 11 nM (serotonin)[1]


[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].

[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.


[Related Small Molecules]

Fluoxetine Hydrochloride | Paroxetine HCl | Vanoxerine dihydrochloride | Sertraline hydrochloride | Fluvoxamine maleat | Fipexide | Duloxetine hydrochloride | Imipramine hydrochloride | Clomipramine HCl | Venlafaxine hydrochloride | Desvenlafaxine succinate | Doxepin hydrochloride | Vortioxetine | Milnacipran ((1S-cis) hydrochloride) | Vilazodone Hydrochloride

Chemical & Physical Properties

[ Molecular Formula ]:
C16H16Cl3N

[ Molecular Weight ]:
328.664

[ Exact Mass ]:
327.034821

[ PSA ]:
26.02000

[ LogP ]:
6.42120

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds