Pharmacology of the GABAA Receptor
作者： Dmytro Berezhnoy , Maria C. Gravielle , David H. Farb
DOI: 10.1002/9780470101001.HCN012
关键词:
摘要: GABA mediates most inhibitory synaptic transmission in the adult vertebrate CNS by activating type-A receptors that contain an integral ion channel and type-B are G-protein coupled. GABAA have been a rich target for development of therapeutics treatment anxiety disorders, convulsive sleep disturbances, induction anesthesia. composed five membrane-spanning subunits, selected from eight subunit subtypes (α, β, γ, δ, η, ρ, π, θ) many which multiple isoforms yielding at least 21 distinct variants. These variations composition can profound effects upon functionality, pharmacology, subcellular distribution receptor subtypes. This chapter focuses on relationship between architecture pharmacology large number clinically relevant compounds such as benzodiazepines, barbiturates, anesthetics, neurosteroids alcohols. Keywords: GABA; ion channels; inhibitory transmission; GABAA receptor; benzodiazepines; barbiturates; anesthetics; neurosteroids; alcohols
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