• Agonists: Main site: Bamaluzole
• Gaboxadol
• Ibotenic acid
• Isoguvacine
• Isonipecotic acid
• Muscimol (Amanita Muscaria)
• Progabide
• SL 75102
• Thiomuscimol
• Tolgabide; Positive allosteric modulators: Barbiturates
• Benzodiazepines
• Carbamates
• Chlormezanone
• Clomethiazole
• Ethanol (Alcohol)
• Etomidate
• Kavalactones (Kava)
• Loreclezole
• Metomidate
• Neuroactive steroids
• Nonbenzodiazepines (β-Carbolines, Cyclopyrrolones, Imidazopyridines, Pyrazolopyrimidines, etc.)
• Phenols
• Piperidinediones
• Propanidid
• Pyrazolopyridines
• Quinazolinones
• ROD-188
• Skullcap
• Stiripentol
• Valerenic acid (Valerian)

Note: See the GABA_A receptor PAMs navbox for a full list of GABA_A positive allosteric modulators.

• Antagonists: Main site: Bicuculline
• Gabazine
• Pitrazepin
• Quisqualamine; Negative allosteric modulators: α5IA
• Bilobalide
• Cicutoxin
• Cyclothiazide
• DMCM
• Flumazenil
• Flurothyl
• Furosemide
• Iomazenil (¹²³I)
• L-655,708
• Oenanthotoxin
• Penicillin
• Pentylenetetrazol
• Picrotoxin
• PWZ-029
• Radequinil
• Ro15-4513
• Sarmazenil
• Suritozole
• Terbequinil
• Thujone
• Thiocolchicoside
• ZK-93426
  

• Agonists: Main site: 1,4-Butanediol
• Baclofen
• GBL
• GHB
• GHV
• GVL
• Lesogaberan
• Phenibut
• Progabide
• SKF-97,541
• Tolgabide; Positive allosteric modulators: BHF-177
• BHFF
• BSPP
• CGP-7930
• GS-39783
  Antagonists: Main site: CGP-35348
• Phaclofen
• Saclofen
• SCH-50911
  

• Agonists: Main site: CACA
• CAMP
• GABOB
• N⁴-Chloroacetylcytosine arabinoside
• Progabide
• Tolgabide
  Antagonists: Main site: Bilobalide
• TPMPA

• Glutamate
• Glutamine
  

• Vitamin B₆ (pyridoxine
• pyridoxamine
• pyridoxal phosphate)
  

• Gabapentin
• Hopantenic acid
• Picamilon
• Pregabalin
• L-Theanine