Properties of GABAA receptor

• Myorelaxant, motor-impairing, and anxiolytic-like properties thought to be mediated by α2, α3, and/or α5 subunits²

  • Benzodiazepines acting on α2, α3, and/or α5 subunits (but NOT α1) have demonstrated nonsedative, nonamnesic anxiolytic properties²

• Anticonvulsant activity and amnesic properties are thought to be mediated by α1 receptors²

• Possible correlation between sensitivity to alcohol and α6 subunit³

• Benzodiazepines and barbiturates bind more strongly when GABA is also bound to the receptor

• Benzodiazepines increase the affinity of the receptor for GABA, and thus increase Cl^­- conductance and hyperpolarizing current

  • Therefore, benzodiazepines are indirect agonists of the GABA receptor

Category: Pharmacology Notes