Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H24N2O4S |
| Molecular Weight | 388.481 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(C=C1)S(=O)(=O)N2CCC[C@H]2C(=O)NC3=CC(C)=CC(C)=C3
InChI
InChIKey=NHPQGZOBHSVTAQ-IBGZPJMESA-N
InChI=1S/C20H24N2O4S/c1-14-11-15(2)13-16(12-14)21-20(23)19-5-4-10-22(19)27(24,25)18-8-6-17(26-3)7-9-18/h6-9,11-13,19H,4-5,10H2,1-3H3,(H,21,23)/t19-/m0/s1
ACT-462206 is a new, potent, and selective dual orexin receptor antagonist that inhibits the stimulating effects of the orexin peptides at both the orexin 1 and 2 receptors. ACT-462206 shows anxiolytic-like properties in rodents without affecting cognition and motor function. It is therefore a potential candidate for the treatment of insomnia and was in phase I of clinical trial, but this research has been discontinued.
CNS Activity
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
891 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24691844 |
1500 mg single, oral dose: 1500 mg route of administration: Oral experiment type: SINGLE co-administered: |
ACT-462206 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27975 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24691844 |
1500 mg single, oral dose: 1500 mg route of administration: Oral experiment type: SINGLE co-administered: |
ACT-462206 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
11.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24691844 |
1500 mg single, oral dose: 1500 mg route of administration: Oral experiment type: SINGLE co-administered: |
ACT-462206 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
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40924317
Created by
admin on Sat Dec 16 11:52:48 GMT 2023 , Edited by admin on Sat Dec 16 11:52:48 GMT 2023
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ACT-462206
Created by
admin on Sat Dec 16 11:52:48 GMT 2023 , Edited by admin on Sat Dec 16 11:52:48 GMT 2023
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PRIMARY | Tocris Cat. No. 5319: ACT 462206Biological Activity: Potent, dual orexin receptor antagonist (IC50 values are 11 and 60 nM for OX2 and OX1 receptors respectively). Exhibits anxiolytic-like properties in vivo. Brain penetrant. | ||
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1361321-96-1
Created by
admin on Sat Dec 16 11:52:48 GMT 2023 , Edited by admin on Sat Dec 16 11:52:48 GMT 2023
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64ONO62P28
Created by
admin on Sat Dec 16 11:52:48 GMT 2023 , Edited by admin on Sat Dec 16 11:52:48 GMT 2023
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ACTIVE MOIETY
