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Details

Stereochemistry ABSOLUTE
Molecular Formula C10H14N2O2
Molecular Weight 194.2304
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Solriamfetol

SMILES

N[C@@H](COC(N)=O)CC1=CC=CC=C1

InChI

InChIKey=UCTRAOBQFUDCSR-SECBINFHSA-N
InChI=1S/C10H14N2O2/c11-9(7-14-10(12)13)6-8-4-2-1-3-5-8/h1-5,9H,6-7,11H2,(H2,12,13)/t9-/m1/s1

HIDE SMILES / InChI

Description

ADX-N05, originally discovered by SK Holdings, is a selective dopamine and norepinephrine reuptake inhibitor (DNRI). ADX-N05 (Solriamfetol, sold under the brand name Sunosi) is approved in the US and is under regulatory review in the EU to improve wakefulness in adult patients with hypersomnia associated with narcolepsy or obstructive sleep apnoea.The US FDA has approved solriamfetol (Sunosi, Jazz Pharmaceuticals) for the treatment of excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea.The dual-acting dopamine and norepinephrine reuptake inhibitor is approved for narcolepsy in once-daily 75 mg and 150 mg doses, and in obstructive sleep apnea in once-daily 37.5 mg, 75 mg, and 150 mg doses.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.9 µM [IC50]
4.4 µM [IC50]

Cmax

ValueDoseCo-administeredAnalytePopulation
499 ng/mL
75 mg single, oral
SOLRIAMFETOL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
5273 ng × h/mL
75 mg single, oral
SOLRIAMFETOL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
7.6 h
75 mg single, oral
SOLRIAMFETOL plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Sample Use Guides

In Vivo Use Guide
The dual-acting dopamine and norepinephrine reuptake inhibitor is approved for narcolepsy in once-daily 75 mg and 150 mg doses, and in obstructive sleep apnea in once-daily 37.5 mg, 75 mg, and 150 mg doses.
Route of Administration: Oral
In Vitro Use Guide
Solriamfetol binds to the dopamine transporter and norepinephrine transporter with low affinity (Ki=14.2 uM and 3.7 uM, respectively), and inhibits the reuptake of dopamine and norepinephrine with low potency (IC50 =2.9 uM and 4.4 uM, respectively). Solriamfetol has no appreciable binding affinity for the serotonin transporter (Ki=81.5 uM) and does not inhibit serotonin reuptake (IC50 > 100 uM).