Stereochemistry | ABSOLUTE |
Molecular Formula | C10H14N2O2 |
Molecular Weight | 194.2304 |
Optical Activity | ( + ) |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
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
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 Target | Pharmacology | Condition | Potency |
---|---|---|---|
2.9 µM [IC50] | |||
4.4 µM [IC50] |
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
Sourcing
PubMed
Sample Use Guides
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
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).