Nomenclature	GABAA
Ensembl Gene family ID	ENSF00000000053
Selective agonists (GABA site)	Muscimol (partial agonist at ρ subunits), isoguvacine (partial agonist at ρ subunits), THIP (gaboxadol; δ subunit preferring, antagonist at ρ subunits), piperidine-4-sulphonic acid (low efficacy at α4 and α6 subunits, antagonist at ρ subunits), isonipecotic acid (α4 and α6 subunit selective via relatively high efficacy, antagonist at ρ subunits), (±)-cis-2-CAMP (ρ subunit selective), 5-MeIAA (ρ subunit selective)
Selective antagonists (GABA site)	Bicuculline (not active at ρ subunits), gabazine (SR95531; weakly active on ρ subunits), TPMPA (ρ subunit selective), cis- and trans-3-ACPBPA (ρ subunit selective), Aza-THIP (ρ subunit selective)
Selective agonists (positive allosteric modulators) (benzodiazepine site)	Diazepam (not α4- or α6-subunits), flunitrazepam (not α4- or α6-subunits), bretazenil (including α4- and α6-subunits, zolpidem, zaleplon and indiplon (α1 subunit selective via high affinity), ocinaplon (α1 subunit selective as essentially a full agonist versus partial agonist at α2, α3 and α5 subunit-containing receptors), L838417 (α2, α3 and α5 subunit selective as a partial agonist versus antagonist at α1-subunit-containing receptors), Ro154513 (selective for α4- and α6-subunit-containing receptors as an agonist versus inverse agonist at α1-, α2-, α3- and α5-subunit-containing receptors), TP003 (selective for α3-subunit-containing receptors as a high efficacy partial agonist versus essentially antagonist activity at α1- α2- and α5-subunit-containing receptors), TPA023 (selective for α2- and α3-subunit-containing receptors as a low efficacy partial agonist versus essentially antagonist activity at α1- and α5-subunit-containing receptors)
Selective antagonists (neutral allosteric modulators) (benzodiazepine site)	Flumazenil (low affinity for α4- or α6-subunits and partial agonist), ZK93426, L838417 (α1 subunit selective via antagonist activity versus partial agonist at α2-, α3- and α5-subunit subunit containing receptors)
Inverse agonists (negative allosteric modulators) (benzodiazepine site)	DMCM, Ro194603, α3IA (α3 selective via higher affinity and greater inverse agonist activity versusα1, α2 and α5-subunit containing receptors), L655708, RY024 (α5 selective via high affinity), α5IA, MRK016 (α5 selective versusα1, α2 and α3-subunit containing receptors via greater inverse agonist efficacy), Ro4938581 (α5 selective versusα1, α2 and α3-subunit containing receptors via higher affinity and greater inverse agonist activity)
Endogenous allosteric modulators	5α-pregnan-3α-ol-20-one (potentiation), tetrahydrodeoxycorticosterone (potentiation), Zn2+ (potent inhibition of receptors formed from binary combinations of α and β subunits, incorporation of a δ- or γ-subunit causes a modest, or pronounced, reduction in inhibitory potency, respectively, Krishek et al., 1998), extracellular protons (subunit dependent activity, Krishek et al., 1996)
Channel blockers	Picrotoxin, TBPS
Probes
GABA site	[3H]Muscimol, [3H]gabazine (SR95531)
benzodiazepine site	[3H]Flunitrazepam (not α4- or α6-subunit), [3H]zolpidem (α1-subunit selective), [3H]L655708 (α5-subunit selective), [3H]RY80 (α5-subunit selective), [3H]Ro154513 [selectively labels α4- and α6-subunit-containing receptors in the presence of a saturating concentration of a ‘classical’ benzodiazepine (e.g., diazepam)], [3H]CGS8216, [11C]flumazenil (PET ligand with low affinity for α4- or α6-subunits), [18F]fluoroethylflumazenil (PET ligand)
Anion channel	[35S]TBPS