GABA analogue
A GABA analogue is a compound which is an analogue or derivative of the neurotransmitter gamma-Aminobutyric acid (GABA) (the IUPAC of which is 4-aminobutanoic acid).
γ-Aminobutyric acid (GABA)
Many GABA analogues are used as drugs, especially as anticonvulsants, sedatives, and anxiolytics,any of the drugs Binds with selective receptor are becomes channel opens
List of GABA analogues
Deaminated
- Butyric acid (butanoic acid) – histone deacetylase inhibitor and full agonist of free fatty acid receptor 2, free fatty acid receptor 3, and 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: valerate (pentanoate), methyl valerate, ethyl valerate, pentyl valerate
- Isovaleric acid (isopentanoic acid/3-methylbutanoic acid) – constituent of valerian; has anticonvulsant effects; PAM of the GABAA receptor
- Derivatives: isovalerate (isopentanoate/3-methylbutanoate), menthyl isovalerate (validolum) – used as an anxiolytic and sedative in Russia
- Isovaleramide (isopentamide/3-methylbutanamide) – constituent of valerian; has anxiolytic and sedative effects; PAM of the GABAA receptor
- Valproic acid (2-propylpentanoic 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 (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- or 4-Hydroxylated
- 3-Hydroxybutanal – synthetic hypnotic and sedative drug
- GHB (γ-hydroxybutyric acid) – neurotransmitter, drug of abuse; agonist of GHB receptor and GABAB 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
- GHBAL (γ-hydroxybutyraldehyde or γ-hydroxybutanal) – 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
β-Substituted
- GABOB (β-hydroxy-GABA) – anticonvulsant; GABA receptor agonist
- Pregabalin (β-isobutyl-GABA) – analgesic, anticonvulsant, anxiolytic, and drug of abuse; potent inhibitor of α2δ subunit-containing VGCCs.
- Phenibut (β-phenyl-GABA) – sedative and anxiolytic from Russia; inhibitor of α2δ subunit-containing VGCCs and, to a lesser extent, GABAB receptor agonist.
- Baclofen (β-(4-chlorophenyl)-GABA) – antispasmodic drug; potent GABAB receptor agonist, weak inhibitor of α2δ subunit-containing VGCCs
- Tolibut (β-(4-methylphenyl)-GABA) – analgesic, tranquilizing, and neuroprotective drug
- Phaclofen (phosphonobaclofen) – GABAB receptor antagonist
- Saclofen (sulfonobaclofen) – GABAB 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 – GABAA receptor agonist
- Guvacine – constituent of areca nuts; GABA reuptake inhibitor
- Isoguvacine – GABAA receptor agonist
- Isonipecotic acid – GABAA receptor partial agonist
- Muscimol – constituent of Amanita muscaria mushrooms; GABAA receptor agonist
- Nipecotic acid – used in scientific research; GABA reuptake inhibitor
GABA prodrugs
Others/miscellaneous
- 1,4-Butanediol – metabolic intermediate and prodrug to GHB
- 3-Methyl-GABA – GABA-T activator
- AABA/homoalanine (α-aminobutyric acid) – used by nonribosomal peptide 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 GABAA 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) – GABAA receptor agonist, GABAB receptor antagonist
- Hopantenic acid (N-pantoyl-GABA) – central nervous system depressant used in Russia
- Isovaline – peripherally selective agonist of the GABAB receptor
- Lesogaberan (AZD-3355) – agonist of the GABAB receptor
- N-Anisoyl-GABA – major active metabolite of the nootropic aniracetam
- NCS-382 – antagonist of the GHB receptor
- Piracetam and other racetams[1] – nootropics
- Pivagabine (N-pivaloyl-GABA) – antidepressant/anxiolytic drug; CRF inhibitor
- Vigabatrin (y-vinyl-GABA) – anticonvulsant; GABA-T inhibitor
See also
References
- John Scott Werry; Michael G. Aman (29 June 2013). Practitioner's Guide to Psychoactive Drugs for Children and Adolescents. Springer Science & Business Media. pp. 415–. ISBN 978-1-4899-0086-9.
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