Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABAAα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned a...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-01, Vol.49 (1), p.35-38
Hauptverfasser:	Goodacre, Simon C, Street, Leslie J, Hallett, David J, Crawforth, James M, Kelly, Sarah, Owens, Andrew P, Blackaby, Wesley P, Lewis, Richard T, Stanley, Joanna, Smith, Alison J, Ferris, Pushpinder, Sohal, Bindi, Cook, Susan M, Pike, Andrew, Brown, Nicola, Wafford, Keith A, Marshall, George, Castro, José L, Atack, John R
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Gabaergic and benzodiazepinic system Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology
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Zusammenfassung:	A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABAAα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm051065l