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ACT-335827

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]

ACT-335827
Clinical data
Routes of
administration
Oral
Drug classOrexin 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
  • 54765113
ChemSpider
  • 30774267
ChEMBL
  • ChEMBL2413367
Chemical and physical data
FormulaC31H38N2O5
Molar mass518.654 g·mol−1
3D model (JSmol)
  • Interactive image
  • 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

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.



335827, orally, available, selective, orexin, receptor, antagonist, with, anxiolytic, effects, animals, unlike, other, orexin, receptor, antagonists, lacks, sedative, effects, found, have, impact, sleep, architecture, mice, clinical, dataroutes, ofadministrati. 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 ACT 335827Clinical dataRoutes ofadministrationOralDrug classOrexin 1 receptor antagonistIdentifiersIUPAC name R 2 S 1 3 4 dimethoxybenzyl 6 7 dimethoxy 3 4 dihydroisoquinolin 2 1H yl N isopropyl 2 phenylacetamidePubChem CID54765113ChemSpider30774267ChEMBLChEMBL2413367Chemical and physical dataFormulaC 31H 38N 2O 5Molar mass518 654 g mol 13D model JSmol Interactive imageSMILES COC1 CC C C H C2 C3 N CCC2 CC OC C3OC C H C NC C C O C4 CC CC C4 CC C1OCInChI 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 s1Key HXHOBPVRRPCTLG SETSBSEESA NReferences Edit 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 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 This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title ACT 335827 amp oldid 1147749538, wikipedia, wiki, book, books, library,

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