ACT-335827

Last updated
ACT-335827
ACT-335827.svg
Clinical data
Routes of
administration 		Oral
Drug class Orexin 1 receptor antagonist
Identifiers
  • (R)-2-((S)-1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-isopropyl-2-phenylacetamide
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C31H38N2O5
Molar mass 518.654 g·mol−1
3D model (JSmol)
  • COC1=CC(C[C@@H](C2=C3)N(CCC2=CC(OC)=C3OC)[C@@H](C(NC(C)C)=O)C4=CC=CC=C4)=CC=C1OC
  • InChI=1S/C31H38N2O5/c1-20(2)32-31(34)30(22-10-8-7-9-11-22)33-15-14-23-18-28(37-5)29(38-6)19-24(23)25(33)16-21-12-13-26(35-3)27(17-21)36-4/h7-13,17-20,25,30H,14-16H2,1-6H3,(H,32,34)/t25-,30+/m0/s1
  • Key:HXHOBPVRRPCTLG-SETSBSEESA-N

ACT-335827 is an orally available, selective orexin 1 receptor antagonist with anxiolytic effects in animals. Unlike other orexin receptor antagonists, ACT-335827 lacks sedative effects and was found to have no impact on sleep architecture in mice. [1] [2]

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<span class="mw-page-title-main">ACT-539313</span> Chemical compound

ACT-539313 is an orexin antagonist medication which is under development for the treatment of binge eating disorder and was previously under development for the treatment of anxiety disorders. It is an orally active small-molecule compound with an elimination half-life of 3.3 to 6.5 hours and acts as a selective orexin OX1 receptor antagonist (1-SORA). As of May 2022, the drug is in phase 2 clinical trials for binge eating disorder. Following negative efficacy results of a phase 2 trial of ACT-539313 for binge eating disorder, Idorsia (the developer of ACT-539313) signaled in May 2022 that it would not pursue further development of the drug for this indication.

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References

  1. ↑ Steiner MA, Gatfield J, Brisbare-Roch C, Dietrich H, Treiber A, Jenck F, Boss C (June 2013). "Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist". ChemMedChem. 8 (6): 898–903. doi:10.1002/cmdc.201300003. PMID   23589487. S2CID   21644009.
  2. ↑ Merlo Pich E, Melotto S (2014). "Orexin 1 receptor antagonists in compulsive behavior and anxiety: possible therapeutic use". Frontiers in Neuroscience. 8: 26. doi: 10.3389/fnins.2014.00026 . PMC   3923148 . PMID   24592206.



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