Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: Improved bioavailability enhances anticonvulsant efficacy

HZ-166 has previously been characterized as an α2,3-selective GABAA receptor modulator with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We discovered a series of ester bioisosteres with reduced metabolic liabilities, leading to improved efficacy as anxiolyt...

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Veröffentlicht in:	Neuropharmacology 2018-07, Vol.137, p.332-343
Hauptverfasser:	Witkin, J.M., Smith, J.L., Ping, X., Gleason, S.D., Poe, M.M., Li, G., Jin, X., Hobbs, J., Schkeryantz, J.M., McDermott, J.S., Alatorre, A.I., Siemian, J.N., Cramer, J.W., Airey, D.C., Methuku, K.R., Tiruveedhula, V.V.N.P.B., Jones, T.M., Crawford, J., Krambis, M.J., Fisher, J.L., Cook, J.M., Cerne, R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alpha 2/3 subunit Anxiety Epilepsy GABA-A receptors
Online-Zugang:	Volltext
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