GABA analogue

A GABA analogue is a compound which is an

IUPAC

of which is 4-aminobutanoic acid).

Many GABA analogues are used as drugs, especially as anticonvulsants, sedatives, and anxiolytics.

List of GABA analogues

niacin receptor 1
- Derivatives:
  butyrate (butanoate), sodium butyrate, methyl butyrate, ethyl butyrate, butyl butyrate, pentyl butyrate

Valeric acid (pentanoic acid) – constituent of valerian; has an unpleasant odor and fruity flavor and esters are used as additives
- Derivatives:
  pentyl valerate
PAM of the GABA_A receptor
- Derivatives:
  isovalerate (isopentanoate/3-methylbutanoate), menthyl isovalerate (validolum) – used as an anxiolytic and sedative in Russia

VDSCs and GABA reuptake, AR/PR antagonist
- Derivatives:
  divalproex sodium, valproate pivoxil

Valpromide (2-propylpentanamide) – anticonvulsant; same mechanism of action as valproic acid, plus inhibitor of epoxide hydrolase
Valnoctamide (2-ethyl-3-methylpentanamide) – anticonvulsant; similar mechanism of action to valproic acid; structural isomer of valpromide

3-Hydroxybutanal – synthetic hypnotic and sedative drug
drug of abuse; agonist of GHB receptor and GABA_B receptor
- Derivatives: sodium oxybate (sodium γ-hydroxybutanoate) – used to treat narcolepsy; same mechanism of action as GHB
Aceburic acid (γ-hydroxybutyric acid acetate) – synthetic prodrug to GHB
GBL (γ-hydroxybutyric acid lactone) – metabolic intermediate
and prodrug to GHB

GHV (γ-hydroxyvaleric acid) – designer drug
; analogue of GHB with similar effects

GVL (γ-valerolactone) – designer drug; prodrug to GHV
T-HCA/GHC
(γ-hydroxycrotonic acid) – neurotransmitter; GHB receptor agonist
GCL
(γ-crotonolactone) – prodrug to T-HCA/GHC
HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) – synthetic GHB receptor agonist
UMB68
(γ-hydroxy-γ-methylpentanoic acid) – synthetic GHB receptor agonist

Baclofen (β-(4-chlorophenyl)-GABA) – antispasmodic drug; potent GABA_B receptor agonist, weak inhibitor of α₂δ subunit-containing VGCCs
neuroprotective
drug
Phaclofen (phosphonobaclofen) – GABA_B receptor antagonist
Saclofen (sulfonobaclofen) – GABA_B receptor antagonist

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
scientific research
; GABA reuptake inhibitor

glutamate
N-Isonicotinoyl-GABA – structural isomer of picamilon
Picamilon (N-nicotinoyl-GABA) – dietary supplement and prescription drug in Russia
Progabide (complex structure) – anticonvulsant
Tolgabide (complex structure) – anticonvulsant

1,4-Butanediol – metabolic intermediate and prodrug to GHB
3-Methyl-GABA – GABA-T activator
synthetases
BABA (β-aminobutyric acid) – known for its ability to induce plant disease resistance

DAVA (δ-aminopentanoic acid) – GABA receptor agonist
Gabamide (γ-aminobutanamide) – GABA receptor agonist
Gabazine (SR-95531) – antagonist of the GABA_A and GHB receptors
GAVA (γ-aminopentanoic acid) – GABA reuptake inhibitor
Glufimet (dimethyl 3-phenylglutamate hydrochloride) – experimental drug related to phenibut
Glutamic acid (glutamate) – neurotransmitter
Homotaurine (tramiprosate) – GABA_A receptor agonist, GABA_B receptor antagonist
Hopantenic acid (N-pantoyl-GABA) – central nervous system depressant used in Russia
Isovaline – peripherally selective agonist of the GABA_B receptor
Lesogaberan (AZD-3355) – 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^[1] – nootropics
CRF
inhibitor
Vigabatrin (y-vinyl-GABA) – anticonvulsant; GABA-T inhibitor

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