ACT-462206
- Investigational
- (2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide
- 1361321-96-1
- 40924317
- 9303
- 34500438
- 64ONO62P28
- ChEMBL3597952
- Interactive image
- O=C(NC=1C=C(C=C(C1)C)C)C2N(CCC2)S(=O)(=O)C3=CC=C(OC)C=C3
- InChI=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
- Key:NHPQGZOBHSVTAQ-IBGZPJMESA-N
ACT-462206 is a dual orexin receptor antagonist (IC50 for OX1 = 60nM, OX2 = 11nM) which has been investigated for the treatment of insomnia. In human trials, ACT-462206 produced dose-dependent sedative effects and was generally well tolerated, with residual sleepiness and headache being the most common adverse events.[1]
Pharmacology
In humans, the sedative effects of ACT-462206 began 45 minutes after oral administration, and dissipated within 8 hours - consistent with a favorable pharmacodynamic profile for the treatment of insomnia. However, the pharmacokinetic profile of ACT-462206 diverges significantly from what would be expected based on behavioral effects. Elevated plasma concentrations of ACT-462206 are sustained for over 24–36 hours after administration - despite behavioral measures of sedation disappearing within 8 hours of administration.[1]
References
- ^ a b Hoch M, van Gorsel H, van Gerven J, Dingemanse J (September 2014). "Entry-into-humans study with ACT-462206, a novel dual orexin receptor antagonist, comparing its pharmacodynamics with almorexant". Journal of Clinical Pharmacology. 54 (9): 979–986. doi:10.1002/jcph.297. PMID 24691844. S2CID 40714628.
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- e
- Agonists: AEX-5
- AEX-19
- AEX-24
- Orexin (A, B)
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- AZD-4041
- C4X-3256 (INDV-2000)
- CR-5542
- CVN-766
- Daridorexant
- Filorexant
- GSK-649868 (SB-649868)
- JNJ-61393215
- Lemborexant
- Nivasorexant (ACT-539313)
- RTIOX-276
- SB-334867
- SB-408124
- Suvorexant
- TCS-1102
- Vornorexant (ORN-0829, TS-142)
- YZJ-1139
- Agonists: AEX-19
- ALKS-2680
- Danavorexton (TAK-925)
- E-2086
- Firazorexton (TAK-994)
- Orexin (A, B)
- SB-668875
- Suntinorexton (TAK-861)
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- Daridorexant
- EMPA
- Filorexant
- GSK-649868 (SB-649868)
- JNJ-10397049
- Lemborexant
- MK-1064
- MK-3697
- MK-8133
- Seltorexant
- Suvorexant
- TCS-1102
- TCS-OX2-29
- Vornorexant (ORN-0829, TS-142)
- YZJ-1139
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