Pharmacology of Mammalian GABAA Receptors

  • Neil Upton
  • Thomas Blackburn
Part of the The Receptors book series (REC)


γ-Aminobutyric acid (GABA) is the most prevalent neurotransmitter in the mammalian brain and exerts its main actions through GABAA receptors (GABAARs). GABAARs have proven to serve as the primary target for many important neuroactive drugs, including benzodiazepines (BZs), barbiturates, steroids, general anesthetics, and possibly ethanol (Macdonald and Olsen, 1994). Recent elegant studies of the molecular nature of GABAARs have revealed the existence of multiple subtypes of these receptors, the composition of which is determined by the formation of pentameric structures from members of at least three distinct subunit families (αl–6, β1–3, γl–3) (Lüddens et al., 1995). Furthermore, by using sophisticated in vitro techniques, the regulation of functional properties by GABA itself, as well as other modulators of GABAARs, has now been shown to differ dramatically with the type of subunit variants in the pentameric complex (Lüddens et al., 1995; Sieghart, 1995).


Partial Agonist Receptor Occupancy Inverse Agonist Full Agonist Neuroactive Steroid 
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