Benzodiazepines

on 23.3.08 with 0 comments



Site of action:

GABAA receptor


Structure of GABAA receptor:


  • Comprised of 5 subunits

    • 2 α subunits (to which GABA binds)

    • 2 β subunits (to which barbiturates bind)

    • 1 γ subunit (to which benzodiazepines bind)

  • Benzodiazepine receptor of GABAA is heterogeneous

    • 13 known subunits of the GABAAγ receptor

      • Benzodiazepine-sensitive

        • α1, α2, α3, α5

      • Benzodiazepine-insensitive

        • α4 and α6

  • Receptor channel contains either positively or neutrally charged amino acid residues that select exclusively for anions (i.e., Cl-)

Category: Pharmacology Notes

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