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Ro4938581

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Ro4938581
Identifiers
  • 3-Bromo-10-(difluoromethyl)-9H-benzo[f]imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]diazepine
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC13H8BrF2N5
Molar mass352.143 g·mol−1
3D model (JSmol)
  • FC(F)C(N=C1)=C(N1C2=C3C=C(Br)C=C2)CN4C3=NC=N4
  • InChI=1S/C13H8BrF2N5/c14-7-1-2-9-8(3-7)13-17-5-19-21(13)4-10-11(12(15)16)18-6-20(9)10/h1-3,5-6,12H,4H2
  • Key:AFJRYPJIKHMNGL-UHFFFAOYSA-N

Ro4938581 is anootropicdrug invented in 2009 by a team working forHoffmann-La Roche, which acts as a subtype-selectiveinverse agonist at theα5 subtype of thebenzodiazepine binding site on theGABAAreceptor. It has good selectivity for the α5 subtype and did not produceconvulsant oranxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivativebasmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation ofcognitive dysfunction inDown syndrome.[4][5]

See also

[edit]

References

[edit]
  1. ^Ballard TM, Knoflach F, Prinssen E, Borroni E, Vivian JA, Basile J, et al. (January 2009). "RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors".Psychopharmacology.202 (1–3):207–23.doi:10.1007/s00213-008-1357-7.PMID 18936916.S2CID 22011375.
  2. ^Knust H, Achermann G, Ballard T, Buettelmann B, Gasser R, Fischer H, et al. (October 2009). "The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction".Bioorganic & Medicinal Chemistry Letters.19 (20):5940–4.doi:10.1016/j.bmcl.2009.08.053.PMID 19762240.
  3. ^Redrobe JP, Elster L, Frederiksen K, Bundgaard C, de Jong IE, Smith GP, et al. (June 2012). "Negative modulation of GABAA α5 receptors by RO4938581 attenuates discrete sub-chronic and early postnatal phencyclidine (PCP)-induced cognitive deficits in rats".Psychopharmacology.221 (3):451–68.doi:10.1007/s00213-011-2593-9.PMID 22124672.S2CID 2550795.
  4. ^Martínez-Cué C, Martínez P, Rueda N, Vidal R, García S, Vidal V, et al. (February 2013)."Reducing GABAA α5 receptor-mediated inhibition rescues functional and neuromorphological deficits in a mouse model of down syndrome".The Journal of Neuroscience.33 (9):3953–66.doi:10.1523/JNEUROSCI.1203-12.2013.PMC 6619314.PMID 23447605.
  5. ^Breindl A (2019)."Inhibiting Inhibition to Treat Down Syndrome Symptoms".BioWorld.
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
1,4-Benzodiazepines
1,5-Benzodiazepines
2,3-Benzodiazepines*
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Thienotriazolodiazepines
Thienobenzodiazepines*
Pyridodiazepines
Pyridotriazolodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Pyrrolobenzodiazepines*
Benzodiazepine prodrugs
* atypical activity profile (notGABAA receptor ligands)


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