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

作者： Simon C. Goodacre , Leslie J. Street , David J. Hallett , James M. Crawforth , Sarah Kelly

关键词: Biochemistry 、 Chemistry 、 Functional selectivity 、 Anxiety disorder 、 Oral administration 、 Binding site 、 Anxiolytic 、 Agonist 、 GABAA receptor 、 Pharmacology 、 Anxiety

摘要: A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog functional selectivity for the GABAAα2 -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g 7-propan-2-olimidazopyrimidine 14k are anxiolytic both conditioned unconditioned animal models anxiety minimal sedation observed at full BZ binding site occupancy.

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

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

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