Dasotraline (hydrochloride)

Modify Date: 2024-01-20 18:25:29

Dasotraline (hydrochloride) Structure
Dasotraline (hydrochloride) structure
Common Name Dasotraline (hydrochloride)
CAS Number 675126-08-6 Molecular Weight 328.664
Density N/A Boiling Point N/A
Molecular Formula C16H16Cl3N Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dasotraline (hydrochloride)


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.

 Names

Name (1R,4S)-N-Desmethyl Sertraline Hydrochloride
Synonym More Synonyms

 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
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.

 Chemical & Physical Properties

Molecular Formula C16H16Cl3N
Molecular Weight 328.664
Exact Mass 327.034821
PSA 26.02000
LogP 6.42120

 Synthetic Route

~94%

Dasotraline (hydrochloride) Structure

Dasotraline (hy...

CAS#:675126-08-6

Literature: Thalen, Lisa K.; Zhao, Dongbo; Sortais, Jean-Baptiste; Paetzold, Jens; Hoben, Christine; Baeckvall, Jan-E. Chemistry - A European Journal, 2009 , vol. 15, # 14 p. 3403 - 3410

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Dasotraline (hydrochloride) Structure

Dasotraline (hy...

CAS#:675126-08-6

Literature: WO2007/6003 A2, ; Page/Page column 26; 29 ;

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Dasotraline (hydrochloride) Structure

Dasotraline (hy...

CAS#:675126-08-6

Literature: Organic Process Research and Development, , vol. 11, # 4 p. 726 - 730

 Synonyms

(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)
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