yana-notes

GABA-A

links: GABA Neuroreceptors reference: @GABAergic deafferentation hypothesis of brain aging and Alzheimer’s disease; pharmacologic profile of the benzodiazepine antagonist, flumazenil (Marczynski 1995) 11-10-2021

GABA-A #

  • Chloride channel heteropentamer; primary target of benzodiazepines. (GABAB is metabotropic.)

Structure #

  • 500
    • Subunits include α1-6, β1-3, γ1-3, δ, ε, θ, π, ρ-3
      • GABA-A-Rho consists entirely of ρ subunits. It’s ubiquitous but is very concentrated in the retina.
    • The ‘Benzodiazepine receptor’ is a binding site situated between a γ and α subunit. The GABA binding site is found between α and β.
    • As you can see, this structure is pretty basic; all the multiplicity in subunit types is perhaps only where γ is (there’s still ρ though) Doesn’t surprise me that not every GABA-A receptor has a benzodiazepine site.