A GABA analogue is a compound which is an
analogue or
derivative
In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. F ...
of the neurotransmitter
gamma-Aminobutyric acid (GABA) (the
IUPAC
The International Union of Pure and Applied Chemistry (IUPAC ) is an international federation of National Adhering Organizations working for the advancement of the chemical sciences, especially by developing nomenclature and terminology. It is ...
of which is 4-aminobutanoic acid).
Many GABA analogues are used as
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
s, especially as
anticonvulsant
Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...
s,
sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but t ...
s, and
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxi ...
s,any of the drugs
Binds with selective receptor are becomes channel opens
List of GABA analogues
Deaminated
*
Butyric acid
Butyric acid (; from grc, βούτῡρον, meaning "butter"), also known under the systematic name butanoic acid, is a straight-chain alkyl carboxylic acid with the chemical formula CH3CH2CH2CO2H. It is an oily, colorless liquid with an unple ...
(butanoic acid) –
histone deacetylase inhibitor
Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases.
HDIs have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics. More recently they are bei ...
and
full agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
of
free fatty acid receptor 2,
free fatty acid receptor 3, and
niacin receptor 1
Hydroxycarboxylic acid receptor 2 (HCA2), also known as niacin receptor 1 (NIACR1) and GPR109A, is a protein which in humans is encoded by the ''HCAR2'' gene. HCA2, like the other hydroxycarboxylic acid receptors HCA1 and HCA3, is a Gi/o-couple ...
** Derivatives:
butyrate
The conjugate acids are in :Carboxylic acids.
{{Commons category, Carboxylate ions, Carboxylate anions
Carbon compounds
Oxyanions ...
(butanoate),
sodium butyrate
Sodium butyrate is a compound with formula Na(C3H7COO). It is the sodium salt of butyric acid. It has various effects on cultured mammalian cells including inhibition of proliferation, induction of differentiation and induction or repression ...
,
methyl butyrate
Methyl butyrate, also known under the systematic name methyl butanoate, is the methyl ester of butyric acid. Like most esters, it has a fruity odor, in this case resembling apples or pineapples. At room temperature, it is a colorless liquid wi ...
,
ethyl butyrate
Ethyl butyrate, also known as ethyl butanoate, or butyric ether, is an ester with the chemical formula CH3CH2CH2COOCH2CH3. It is soluble in propylene glycol, paraffin oil, and kerosene. It has a fruity odor, similar to pineapple, and is a key in ...
,
butyl butyrate,
pentyl butyrate
*
Valeric acid
Valeric acid or pentanoic acid is a straight-chain alkyl carboxylic acid with the chemical formula . Like other low-molecular-weight carboxylic acids, it has an unpleasant odor. It is found in the perennial flowering plant ''Valeriana officina ...
(pentanoic acid) – constituent of valerian; has an unpleasant odor and fruity flavor and esters are used as additives
** Derivatives:
valerate
Valeric acid or pentanoic acid is a straight-chain alkyl carboxylic acid with the chemical formula . Like other low-molecular-weight carboxylic acids, it has an unpleasant odor. It is found in the perennial flowering plant ''Valeriana officina ...
(pentanoate),
methyl valerate,
ethyl valerate
Ethyl pentanoate, also commonly known as ethyl valerate, is an organic compound used in flavors. It is an ester with the molecular formula C7H14O2. This colorless liquid is poorly soluble in water but miscible with organic solvents.
As is the c ...
,
pentyl valerate
Pentyl pentanoate (C4H9COOC5H11) is an ester used in dilute solution to replicate the scent or flavour of apple, and sometimes pineapple
The pineapple (''Ananas comosus'') is a tropical plant with an edible fruit; it is the most economically ...
*
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
Russia (, , ), or the Russian Federation, is a List of transcontinental countries, transcontinental country spanning Eastern Europe and North Asia, Northern Asia. It is the List of countries and dependencies by area, largest country in the ...
*
Isovaleramide
Isovaleramide is an organic compound with the formula (CH3)2CHCH2C(O)NH2. The amide derived from isovaleric acid, it is a colourless solid.
Occurrence and biological activity
Isovaleramide is a constituent of valerian root.
In humans, it acts a ...
(isopentamide/3-methylbutanamide) – constituent of
valerian; has anxiolytic and sedative effects;
PAM of the
GABAA receptor
*
Valproic acid
Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches. They are useful for the prevention of seizures in those ...
(2-propylpentanoic acid) – anticonvulsant/
mood stabilizer
A mood stabilizer is a psychiatric medication used to treat mood disorders characterized by intense and sustained mood shifts, such as bipolar disorder and the bipolar type of schizoaffective disorder.
Uses
Mood stabilizers are best known for th ...
;
inhibitor of
HDAC
Histone deacetylases (, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around h ...
,
SSADH, and
GABA-T,
blocker of
VDSCs and
GABA reuptake,
AR/
PR antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
** Derivatives:
sodium valproate
Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches. They are useful for the prevention of seizures in those ...
,
valproate semisodium
Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches. They are useful for the prevention of seizures in thos ...
,
divalproex sodium
Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches. They are useful for the prevention of seizures in thos ...
,
valproate pivoxil
*
Valpromide
Valpromide (marketed as Depamide by Sanofi-Aventis) is a carboxamide derivative of valproic acid used in the treatment of epilepsy and some affective disorder
Affect, in psychology, refers to the underlying experience of feeling, emotion ...
(2-propylpentanamide) – anticonvulsant; same mechanism of action as valproic acid, plus inhibitor of
epoxide hydrolase
Epoxide hydrolases (EH's), also known as epoxide hydratases, are enzymes that metabolize compounds that contain an epoxide residue; they convert this residue to two hydroxyl residues through an epoxide hydrolysis reaction to form diol products. ...
*
Valnoctamide
Valnoctamide ( INN, USAN) has been used in France as a sedative-hypnotic since 1964. It is a structural isomer of valpromide, a valproic acid prodrug; unlike valpromide, however, valnoctamide is not transformed into its homologous acid, valnoct ...
(2-ethyl-3-methylpentanamide) – anticonvulsant; similar mechanism of action to valproic acid; structural isomer of valpromide
3- or 4-Hydroxylated
*
3-Hydroxybutanal – synthetic
hypnotic
Hypnotic (from Greek ''Hypnos'', sleep), or soporific drugs, commonly known as sleeping pills, are a class of (and umbrella term for) psychoactive drugs whose primary function is to induce sleep (or surgical anesthesiaWhen used in anesthesia ...
and
sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but t ...
drug
*
GHB
''gamma''-Hydroxybutyric acid (or γ-hydroxybutyric acid (GHB), also known as 4-hydroxybutanoic acid) is a naturally occurring neurotransmitter and a depressant drug. It is a precursor to GABA, glutamate, and glycine in certain brain areas. ...
(γ-hydroxybutyric acid) –
neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell.
Neuro ...
,
drug of abuse
Substance abuse, also known as drug abuse, is the use of a drug in amounts or by methods which are harmful to the individual or others. It is a form of substance-related disorder. Differing definitions of drug abuse are used in public health, ...
; agonist of
GHB receptor
The γ-hydroxybutyrate (GHB) receptor (GHBR), originally identified as GPR172A, is an excitatory G protein-coupled receptor (GPCR) that binds the neurotransmitter and psychoactive drug γ-hydroxybutyric acid (GHB). As solute carrier family 52 m ...
and
GABAB receptor
** Derivatives:
sodium oxybate
Sodium oxybate, sold under the brand name Xyrem among others, is a medication used to treat two symptoms of narcolepsy: sudden muscle weakness and excessive daytime sleepiness. It is used sometimes in France and Italy as an anesthetic given i ...
(sodium γ-hydroxybutanoate) – used to treat
narcolepsy
Narcolepsy is a long-term neurological disorder that involves a decreased ability to regulate sleep–wake cycles. Symptoms often include periods of excessive daytime sleepiness and brief involuntary sleep episodes. About 70% of those affec ...
; same
mechanism of action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targe ...
as GHB
*
Aceburic acid (γ-hydroxybutyric acid acetate) – synthetic
prodrug
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...
to GHB
*
GBL (γ-hydroxybutyric acid lactone) –
metabolic intermediate
Metabolic intermediates are molecules that are the precursors or metabolites of biologically significant molecules.
Although these intermediates are of relatively minor direct importance to cellular function, they can play important roles in the a ...
and prodrug to GHB
*
GHBAL (γ-hydroxybutyraldehyde or γ-hydroxybutanal) – metabolic intermediate and prodrug to GHB
*
GHV (γ-hydroxyvaleric acid) –
designer drug
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Des ...
; 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
γ-Amino-β-hydroxybutyric acid (GABOB), also known as β-hydroxy-γ-aminobutyric acid (β-hydroxy-GABA), and sold under the brand name Gamibetal among others, is an anticonvulsant which is used for the treatment of epilepsy in Europe, Japan, and ...
(β-hydroxy-GABA) – anticonvulsant;
GABA receptor agonist
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. There are three ...
*
Pregabalin
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic and anxiolytic medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome, opioid withdrawal and generalized anxiety disord ...
(β-isobutyl-GABA) –
analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...
,
anticonvulsant
Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...
,
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxi ...
, and
drug of abuse
Substance abuse, also known as drug abuse, is the use of a drug in amounts or by methods which are harmful to the individual or others. It is a form of substance-related disorder. Differing definitions of drug abuse are used in public health, ...
; 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, GABA
B receptor agonist.
*
Baclofen
Baclofen, sold under the brand name Lioresal among others, is a medication used to treat muscle spasticity such as from a spinal cord injury or multiple sclerosis. It may also be used for hiccups and muscle spasms near the end of life. It is ta ...
(β-(4-chlorophenyl)-GABA) –
antispasmodic
An antispasmodic (synonym: spasmolytic) is a pharmaceutical drug or other agent that suppresses muscle spasms.
Smooth muscle spasm
One type of antispasmodics is used for smooth muscle relaxation, especially in tubular organs of the gastrointesti ...
drug; potent GABA
B receptor agonist, weak inhibitor of α
2δ subunit-containing VGCCs
*
Tolibut (β-(4-methylphenyl)-GABA) – analgesic,
tranquilizing, and
neuroprotective
Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal los ...
drug
*
Phaclofen (phosphonobaclofen) – GABA
B receptor antagonist
*
Saclofen (sulfonobaclofen) – GABA
B receptor antagonist
Cyclized
*
Arecaidine
Arecaidine is a bio-active alkaloid in areca nuts. It is a competitive GABA uptake inhibitor. Lime is said to hydrolyse arecoline
Arecoline () is a nicotinic acid-based mild parasympathomimetic stimulant alkaloid found in the areca nut, the f ...
– constituent of
areca nuts
''Areca'' is a genus of 51 species of palms in the family Arecaceae, found in humid tropical forests from the islands of the Philippines, Malaysia and India, across Southeast Asia to Melanesia. The generic name ''Areca'' is derived from a name u ...
; GABA reuptake inhibitor
*
Gabaculine –
neurotoxin
Neurotoxins are toxins that are destructive to nerve tissue (causing neurotoxicity). Neurotoxins are an extensive class of exogenous chemical neurological insultsSpencer 2000 that can adversely affect function in both developing and mature ner ...
; GABA-T inhibitor and
GABA reuptake inhibitor
A GABA reuptake inhibitor (GRI) is a type of drug which acts as a reuptake inhibitor for the neurotransmitter gamma-Aminobutyric acid (GABA) by blocking the action of the gamma-Aminobutyric acid transporters (GATs). This in turn leads to incre ...
*
Gabapentin
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat partial seizures and neuropathic pain. It is a first-line medication for the treatment of neuropathic pain caused by diabet ...
– anticonvulsant; inhibitor of α
2δ subunit-containing VGCCs
**
Gabapentin enacarbil
Gabapentin enacarbil (Horizant () (), Regnite (in Japan)) is an anticonvulsant and analgesic drug of the gabapentinoid class, and a prodrug to gabapentin. It was designed for increased oral bioavailability over gabapentin, and human trials show ...
– used for the treatment of
restless legs syndrome
Restless legs syndrome (RLS), also known as Willis-Ekbom disease (WED), is generally a long-term disorder that causes a strong urge to move one's legs. There is often an unpleasant feeling in the legs that improves somewhat by moving them. This ...
and
postherpetic neuralgia
Postherpetic neuralgia (PHN) is neuropathic pain that occurs due to damage to a peripheral nerve caused by the reactivation of the varicella zoster virus (herpes zoster, also known as shingles). Typically, the nerve pain (neuralgia) is confined t ...
; same mechanism of action as gabapentin
*
Gaboxadol
Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP), is a conformationally constrained derivative of the alkaloid muscimol that was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-Larsen. In the early 19 ...
– GABA
A receptor agonist
*
Guvacine
Guvacine is an pyridine alkaloid in areca nuts. It is the ''N''-demethylated derivative
In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to ...
– constituent of areca nuts; GABA reuptake inhibitor
*
Isoguvacine
Isoguvacine is a GABAA receptor agonist used in scientific research.
See also
* Gaboxadol
* Muscimol
Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of '' Amanita muscaria'' and related specie ...
– GABA
A receptor agonist
*
Isonipecotic acid – GABA
A receptor
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...
*
Muscimol
Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of '' Amanita muscaria'' and related species of mushroom. Muscimol is a potent and selective orthosteric agonist for the GABAA receptors and displa ...
– constituent of ''
Amanita muscaria
''Amanita muscaria'', commonly known as the fly agaric or fly amanita, is a basidiomycete of the genus ''Amanita''. It is also a muscimol mushroom. Native throughout the temperate and boreal regions of the Northern Hemisphere, ''Amanita muscar ...
'' mushrooms; GABA
A receptor agonist
*
Nipecotic acid
Nipecotic acid is a GABA uptake inhibitor used in scientific research.
See also
* Deramciclane
* Tiagabine
Tiagabine (trade name Gabitril) is an anticonvulsant medication produced by Cephalon that is used in the treatment of epilepsy. The ...
– used in
scientific research
The scientific method is an empirical method for acquiring knowledge that has characterized the development of science since at least the 17th century (with notable practitioners in previous centuries; see the article history of scientific m ...
; GABA reuptake inhibitor
GABA prodrugs
*
L-Glutamine – endogenous
precursor
Precursor or Precursors may refer to:
* Precursor (religion), a forerunner, predecessor
** The Precursor, John the Baptist
Science and technology
* Precursor (bird), a hypothesized genus of fossil birds that was composed of fossilized parts of u ...
of GABA and
glutamate
Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can syn ...
*
N-Isonicotinoyl-GABA – structural isomer of
picamilon
*
Picamilon (N-nicotinoyl-GABA) – dietary supplement and prescription drug in Russia
*
Progabide
Progabide (INN; trade name Gabrene, Sanofi-Aventis) is an analogue and prodrug of γ-aminobutyric acid (GABA) used in the treatment of epilepsy. Via conversion into GABA, progabide behaves as an agonist of the GABAA, GABAB, and GABAA-ρ re ...
(complex structure) – anticonvulsant
*
Tolgabide
Tolgabide (INN; development code SL-81.0142) is a drug which was patented by Synthélabo as an anticonvulsant but was never marketed. It is an analogue of progabide and acts similarly to it as a prodrug of GABA, and therefore as an indirect ...
(complex structure) – anticonvulsant
Others/miscellaneous
*
1,4-Butanediol
1,4-Butanediol, colloquially known as BD or BDO, is a primary alcohol, and an organic compound, with the formula HOCH2CH2CH2CH2OH. It is a colorless viscous liquid. It is one of four stable isomers of butanediol.
Synthesis
In industrial sy ...
– metabolic intermediate and prodrug to GHB
*
3-Methyl-GABA – GABA-T activator
*
AABA/homoalanine (α-aminobutyric acid) – used by
nonribosomal peptide Nonribosomal peptides (NRP) are a class of peptide secondary metabolites, usually produced by microorganisms like bacteria and fungi. Nonribosomal peptides are also found in higher organisms, such as nudibranchs, but are thought to be made by bacter ...
synthetase
In biochemistry, a ligase is an enzyme that can catalyze the joining (Ligation (molecular biology), ligation) of two large molecules by forming a new chemical bond. This is typically via hydrolysis of a small pendant chemical group on one of the ...
s
*
BABA (β-aminobutyric acid) – known for its ability to induce
plant disease resistance
Plant disease resistance protects plants from pathogens in two ways: by pre-formed structures and chemicals, and by infection-induced responses of the immune system. Relative to a susceptible plant, disease resistance is the reduction of pathoge ...
*
DAVA (δ-aminopentanoic acid) – GABA receptor agonist
*
Gabamide (γ-aminobutanamide) – GABA receptor agonist
*
Gabazine
Gabazine (SR-95531) is a drug that acts as an Receptor antagonist, antagonist at GABAA receptor, GABAA Receptor (biochemistry), receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsio ...
(SR-95531) – antagonist of the GABA
A and GHB receptors
*
GAVA (γ-aminopentanoic acid) – GABA reuptake inhibitor
*
Glufimet
Glufimet (developmental code name RGPU-238), also known as dimethyl 3-phenylglutamate hydrochloride, is a derivative of glutamic acid (glutamate) which was developed in Russia and is related to the γ-aminobutyric acid (GABA) derivative phenibut ...
(dimethyl 3-phenylglutamate hydrochloride) – experimental drug related to phenibut
*
Glutamic acid
Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can synt ...
(glutamate) – neurotransmitter
*
Homotaurine
Homotaurine (also known as tramiprosate ( INN), 3-amino-1-propanesulfonic acid, or 3-APS) is a natural sulfonic acid found in seaweed. It is analogous to taurine, but with an extra carbon in its chain. It has GABAergic activity, apparently by mim ...
(tramiprosate) – GABA
A receptor agonist, GABA
B receptor antagonist
*
Hopantenic acid
Hopantenic acid (homopantothenic acid), also known as N-pantoyl-GABA, is a central nervous system depressant. Formulated as the calcium salt, it is used as a pharmaceutical drug in the Russian Federation for a variety of neurological, psychologic ...
(N-pantoyl-GABA) –
central nervous system depressant
A depressant, or central depressant, is a drug that lowers neurotransmission levels, which is to depress or reduce arousal or stimulation, in various areas of the brain. Depressants are also colloquially referred to as downers as they lower the l ...
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
Piracetam is a drug marketed as a treatment for myoclonus. It is also used as a cognitive enhancer to improve memory, attention, and learning. Evidence to support its use is unclear, with some studies showing modest benefits in specific populat ...
and other
racetam
Racetams are a class of drugs that share a pyrrolidone nucleus. Some, such as piracetam, aniracetam, oxiracetam, pramiracetam and phenylpiracetam are considered nootropics. Others such as levetiracetam, brivaracetam, and seletracetam are ant ...
s
– nootropics
*
Pivagabine
Pivagabine ( INN; brand name Tonerg), also known as ''N''-pivaloyl-γ-aminobutyric acid or ''N''-pivaloyl-GABA, is an antidepressant and anxiolytic drug which was introduced in Italy in 1997 for the treatment of depressive and maladaptive syndro ...
(N-pivaloyl-GABA) –
antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
/anxiolytic drug;
CRF inhibitor
*
Vigabatrin
Vigabatrin, brand name Sabril, is a medication used to treat epilepsy. It became available as a generic medication in 2019.
It works by inhibiting the breakdown of γ-aminobutyric acid (GABA). It is also known as γ-vinyl-GABA, and is a stru ...
(y-vinyl-GABA) – anticonvulsant; GABA-T inhibitor
See also
*
Bamaluzole
*
Bicuculline
Bicuculline is a phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from ''Dicentra cucullaria'', '' Adlumia ...
*
Deramciclane
*
Ethanol
Ethanol (abbr. EtOH; also called ethyl alcohol, grain alcohol, drinking alcohol, or simply alcohol) is an organic compound. It is an Alcohol (chemistry), alcohol with the chemical formula . Its formula can be also written as or (an ethyl ...
*
Fengabine
*
Gabapentinoid
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which block α2δ subunit-containing voltage-dependent calcium ch ...
*
Loreclezole
*
Propofol
Propofol, marketed as Diprivan, among other names, is a short-acting medication that results in a decreased level of consciousness and a lack of memory for events. Its uses include the starting and maintenance of general anesthesia, sedation f ...
*
Retigabine/ezogabine
*
Tiagabine
Tiagabine (trade name Gabitril) is an anticonvulsant medication produced by Cephalon that is used in the treatment of epilepsy. The drug is also used off-label in the treatment of anxiety disorders and panic disorder.
Medical uses
Tiagabine is a ...
*
Valerenic acid
Valerenic acid is a sesquiterpenoid constituent of the essential oil of the valerian plant.
Valerian is used as a herbal sedative which may be helpful in the treatment of insomnia. Valerenic acid may be at least partly responsible for valeri ...
References
{{Channel blockers
GABA receptor agonists