Differentiating the role of γ-aminobutyric acid type A (GABAA) receptor subtypes

摘要: The inhibitory tone maintained throughout the central nervous system relies predominantly on activity of neuronal GABAA (gamma-aminobutyric acid type A) receptors. This receptor family comprises various subtypes that have unique regional distributions, but little is known about role played by each subtype. majority receptors contain a gamma2 subunit and are sensitive to modulation BZs (benzodiazepines), differ with regard alpha beta subunits. Mutagenesis studies combined molecular modelling enabled greater understanding structure dynamics. can now be extended in vivo through translation genetically modified mice containing these mutations. Ideally, mutation should leave normal function intact, this case mutations affecting BZ-binding site receptor. We generated mutations, which affect BZ different subunits, enable discrimination behavioural consequences drug action. has aided our roles individual particular behaviours. also used technique explore subunits conferring anaesthetic etomidate. together development subtype-selective compounds facilitates