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 GABA A agonists for the …

…, DS Reynolds, A Pike, KA Wafford, R Newman…

Index: Goodacre, Simon C.; Hallett, David J.; Carling, Robert W.; Castro, Jose L.; Reynolds, David S.; Pike, Andrew; Wafford, Keith A.; Newman, Robert; Atack, John R.; Street, Leslie J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1582 - 1585

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Citation Number: 18

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.