GABA analogue

List of GABA analogues

Deaminated

• Butyric acid – histone deacetylase inhibitor and full agonist of free [fatty acid receptor 2], free fatty acid receptor 3, and niacin receptor 1
• * Derivatives: butyrate, sodium butyrate, methyl butyrate, ethyl butyrate, butyl butyrate, pentyl butyrate
• Valeric acid – constituent of valerian; has an unpleasant odor and fruity flavor and esters are used as additives
• * Derivatives: valerate, methyl valerate, ethyl valerate, pentyl valerate
• Isovaleric acid – constituent of valerian; has anticonvulsant effects; PAM of the GABA_A receptor
• * Derivatives: isovalerate, menthyl isovalerate – used as an anxiolytic and sedative in Russia
• Isovaleramide – constituent of valerian; has anxiolytic and sedative effects; PAM of the GABA_A receptor
• Valproic acid – anticonvulsant/mood stabilizer; inhibitor of HDAC, SSADH, and GABA-T, blocker of VDSCs and GABA reuptake, AR/PR antagonist
• * Derivatives: sodium valproate, valproate semisodium, divalproex sodium, valproate pivoxil
• Valpromide – anticonvulsant; same mechanism of action as valproic acid, plus inhibitor of epoxide hydrolase
• Valnoctamide – anticonvulsant; similar mechanism of action to valproic acid; structural isomer of valpromide

3- or 4-Hydroxylated

• 3-Hydroxybutanal – synthetic hypnotic and sedative drug
• GHB – neurotransmitter, drug of abuse; agonist of GHB receptor and GABA_B receptor
• * Derivatives: sodium oxybate – used to treat narcolepsy; same mechanism of action as GHB
• Aceburic acid – synthetic prodrug to GHB
• GBL – metabolic intermediate and prodrug to GHB
• GHBAL – metabolic intermediate and prodrug to GHB
• GHV – designer drug; analogue of GHB with similar effects
• GVL – designer drug; prodrug to GHV
• T-HCA/GHC – neurotransmitter; GHB receptor agonist
• GCL – prodrug to T-HCA/GHC
• HOCPCA – synthetic GHB receptor agonist
• UMB68 – synthetic GHB receptor agonist

β-Substituted

• GABOB – anticonvulsant; GABA receptor agonist
• Pregabalin – analgesic, anticonvulsant, and anxiolytic; potent inhibitor of α₂δ subunit-containing VGCCs.
• Phenibut – sedative and anxiolytic from Russia; GABA_B receptor agonist, and to a lesser extent inhibitor of α₂δ subunit-containing VGCCs.
• Baclofen – antispasmodic drug; potent GABA_B receptor agonist, weak inhibitor of α₂δ subunit-containing VGCCs
• Tolibut – analgesic, tranquilizing, and neuroprotective drug
• Phaclofen – GABA_B receptor antagonist
• Saclofen – GABA_B receptor antagonist

Cyclized

• Arecaidine – constituent of areca nuts; GABA reuptake inhibitor
• Gabaculine – neurotoxin; GABA-T inhibitor and GABA reuptake inhibitor
• Gabapentin – anticonvulsant; inhibitor of α₂δ subunit-containing VGCCs
• * Gabapentin enacarbil – used for the treatment of restless legs syndrome and postherpetic neuralgia; same mechanism of action as gabapentin
• Gaboxadol – GABA_A receptor agonist
• Guvacine – constituent of areca nuts; GABA reuptake inhibitor
• Isoguvacine – GABA_A receptor agonist
• Isonipecotic acid – GABA_A receptor partial agonist
• Muscimol – constituent of Amanita muscaria mushrooms; GABA_A receptor agonist
• Nipecotic acid – used in scientific research; GABA reuptake inhibitor

GABA prodrugs

• L-Glutamine – endogenous precursor of GABA and glutamate
• N-Isonicotinoyl-GABA – structural isomer of picamilon
• Picamilon – dietary supplement and prescription drug in Russia
• Progabide – anticonvulsant
• Tolgabide – anticonvulsant

Others/miscellaneous

• 1,4-Butanediol – metabolic intermediate and prodrug to GHB
• 3-Methyl-GABA – GABA-T activator
• AABA/homoalanine – used by nonribosomal peptide synthetases
• BABA – known for its ability to induce plant disease resistance
• DAVA – GABA receptor agonist
• Gabamide – GABA receptor agonist
• Gabazine – antagonist of the GABA_A and GHB receptors
• GAVA – GABA reuptake inhibitor
• Glufimet – experimental drug related to phenibut
• Glutamic acid – neurotransmitter
• Homotaurine – GABA_A receptor agonist, GABA_B receptor antagonist
• Hopantenic acid – central nervous system depressant used in Russia
• Isovaline – peripherally selective agonist of the GABA_B receptor
• Lesogaberan – agonist of the GABA_B receptor
• N-Anisoyl-GABA – major active metabolite of the nootropic aniracetam
• NCS-382 – antagonist of the GHB receptor
• Piracetam and other racetams – nootropics
• Pivagabine – antidepressant/anxiolytic drug; CRF inhibitor
• Vigabatrin – anticonvulsant; GABA-T inhibitor