Ro4938581

Ro4938581
Nome IUPAC
	3-Bromo-10-(difluoromethyl)-9H-benzo[f]imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]diazepine
Caratteristiche generali
Formula bruta o molecolare	C13H8BrF2N5
Massa molecolare (u)	352,143 g/mol
PubChem	11624499
SMILES	C1C2=C(N=CN2C3=C(C=C(C=C3)Br)C4=NC=NN41)C(F)F
Dati farmacocinetici
Metabolismo	Epatico
Escrezione	renale
Indicazioni di sicurezza

L'Ro4938581 è uno psicofarmaco appartenente alla categoria delle benzodiazepine inventato nel 2009 dalla casa farmaceutica Hoffmann-La Roche, che agisce come un sottotipo-selettivo agonista del recettore GABA A α5. Non produce effetti convulsivi o ansiogeni negli studi sugli animali, il che lo rende un potenziale nootropico.^[1]^[2]^[3] Ro4938581 è un derivato correlato del basmisanil (RG-1662, RO5186582) ed è stato successivamente testato per alleviare la disfunzione cognitiva nella sindrome di Down.^[4]^[5]

Note

^ Ballard TM, Knoflach F, Prinssen E, Borroni E, Vivian JA, Basile J, Gasser R, Moreau JL, Wettstein JG, Buettelmann B, Knust H, Thomas AW, Trube G, Hernandez MC, RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors, in Psychopharmacology, vol. 202, 1–3, gennaio 2009, pp. 207-23, DOI:10.1007/s00213-008-1357-7, PMID 18936916.
^ Knust H, Achermann G, Ballard T, Buettelmann B, Gasser R, Fischer H, Hernandez MC, Knoflach F, Koblet A, Stadler H, Thomas AW, Trube G, Waldmeier P, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction, in Bioorganic & Medicinal Chemistry Letters, vol. 19, n. 20, ottobre 2009, pp. 5940-4, DOI:10.1016/j.bmcl.2009.08.053, PMID 19762240.
^ Redrobe JP, Elster L, Frederiksen K, Bundgaard C, de Jong IE, Smith GP, Bruun AT, Larsen PH, Didriksen M, Negative modulation of GABAA α5 receptors by RO4938581 attenuates discrete sub-chronic and early postnatal phencyclidine (PCP)-induced cognitive deficits in rats, in Psychopharmacology, vol. 221, n. 3, giugno 2012, pp. 451-68, DOI:10.1007/s00213-011-2593-9, PMID 22124672.
^ Martínez-Cué C, Martínez P, Rueda N, Vidal R, García S, Vidal V, Corrales A, Montero JA, Pazos Á, Flórez J, Gasser R, Thomas AW, Honer M, Knoflach F, Trejo JL, Wettstein JG, Hernández MC, Reducing GABAA α5 receptor-mediated inhibition rescues functional and neuromorphological deficits in a mouse model of down syndrome, in The Journal of Neuroscience, vol. 33, n. 9, febbraio 2013, pp. 3953-66, DOI:10.1523/JNEUROSCI.1203-12.2013, PMC 6619314, PMID 23447605.
^ Anette Breindl, Inhibiting Inhibition to Treat Down Syndrome Symptoms, in BioWorld, 2019.

Voci correlate

Portale Chimica

Portale Medicina

[1] Ballard TM, Knoflach F, Prinssen E, Borroni E, Vivian JA, Basile J, Gasser R, Moreau JL, Wettstein JG, Buettelmann B, Knust H, Thomas AW, Trube G, Hernandez MC, RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors, in Psychopharmacology, vol. 202, 1–3, gennaio 2009, pp. 207-23, DOI:10.1007/s00213-008-1357-7, PMID 18936916.

[2] Knust H, Achermann G, Ballard T, Buettelmann B, Gasser R, Fischer H, Hernandez MC, Knoflach F, Koblet A, Stadler H, Thomas AW, Trube G, Waldmeier P, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction, in Bioorganic & Medicinal Chemistry Letters, vol. 19, n. 20, ottobre 2009, pp. 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, Bruun AT, Larsen PH, Didriksen M, Negative modulation of GABAA α5 receptors by RO4938581 attenuates discrete sub-chronic and early postnatal phencyclidine (PCP)-induced cognitive deficits in rats, in Psychopharmacology, vol. 221, n. 3, giugno 2012, pp. 451-68, DOI:10.1007/s00213-011-2593-9, PMID 22124672.

[4] Martínez-Cué C, Martínez P, Rueda N, Vidal R, García S, Vidal V, Corrales A, Montero JA, Pazos Á, Flórez J, Gasser R, Thomas AW, Honer M, Knoflach F, Trejo JL, Wettstein JG, Hernández MC, Reducing GABAA α5 receptor-mediated inhibition rescues functional and neuromorphological deficits in a mouse model of down syndrome, in The Journal of Neuroscience, vol. 33, n. 9, febbraio 2013, pp. 3953-66, DOI:10.1523/JNEUROSCI.1203-12.2013, PMC 6619314, PMID 23447605.

[5] Anette Breindl, Inhibiting Inhibition to Treat Down Syndrome Symptoms, in BioWorld, 2019.

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