Title of article :
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety
Author/Authors :
Simon C. Goodacre، نويسنده , , David J. Hallett، نويسنده , , Robert W. Carling، نويسنده , , José L. Castro، نويسنده , , David S. Reynolds، نويسنده , , Andrew Pike، نويسنده , , Keith A. Wafford، نويسنده , , Robert Newman، نويسنده , , John R. Atack، نويسنده , , Leslie J. Street، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
Abstract :
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and α3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy.
Keywords :
2-a]pyrazin-8-ones , 2 , 4]triazin-8-ones , 2 , 4]triazin-8-ones , GABAA agonists , Functionally selective for GABAA?2 and ?3 , Anxiolytic
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
