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Ionotropic receptor and ligand-gated ion channel
The GABAA receptor (GABAAR) is an ionotropic receptor (i.e., ligand-gated ion channel). Its endogenous ligand is γ-aminobutyric acid (GABA), the major
GABAA_receptor
Class of neurotransmitter modulators
In pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator
GABAA receptor positive allosteric modulator
GABAA_receptor_positive_allosteric_modulator
Class of transport proteins
GABAA-rho receptor (previously known as the GABAC receptor) is a subclass of GABAA receptors composed entirely of rho (ρ) subunits. GABAA receptors including
GABAA-rho_receptor
Hallucinogenic drug
A GABAA receptor agonist is a drug that acts as an orthosteric agonist of the GABAA receptor, the major signaling receptor of the inhibitory neurotransmitter
GABAA_receptor_agonist
Receptors that respond to gamma-aminobutyric acid
of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors); whereas GABAB receptors are G protein-coupled
GABA_receptor
Investigational insomnia drugs
lorazepam (benzodiazepine and GABAA receptor positive allosteric modulator), and zolpidem (nonbenzodiazepine/Z-drug and GABAA receptor positive allosteric modulator)
List of investigational insomnia drugs
List_of_investigational_insomnia_drugs
Drug Class
and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other agents which may have GABAA receptor antagonism include the antibiotic ciprofloxacin
GABA_receptor_antagonist
Investigational generalized anxiety disorder drugs
dopamine D2 and D3 receptor partial agonist and other actions [7] ENX-102 (ENX102) — α2, α3, and α5 subunit-containing GABAA receptor positive allosteric
List of investigational generalized anxiety disorder drugs
List_of_investigational_generalized_anxiety_disorder_drugs
Drug class
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel
GABAA receptor negative allosteric modulator
GABAA_receptor_negative_allosteric_modulator
Category of drug
anticonvulsant, and muscle relaxant effects. There are three receptors of GABA. The GABAA and GABAA-ρ receptors are ion channels that are permeable to chloride ions
GABA_receptor_agonist
levomethorphan, and nalorphine Others such as spiradoline, enadoline, and HZ-2 GABAA receptor agonists with hallucinogenic effects include the following: Muscimol
List_of_hallucinogens
Drug whose use induces sleep
for all older patients. Their mechanism of action is primarily at GABAA receptors. Nonbenzodiazepines (Z-drugs) are a class of psychoactive drugs that
Hypnotic
Investigational anxiety disorder drugs
acetylcholine receptor negative allosteric modulator [3] BAER-101 (AZ-7325; AZD-7325) – selective GABAA α2 and α3 subunit-containing receptor positive allosteric
List of investigational anxiety disorder drugs
List_of_investigational_anxiety_disorder_drugs
Naturally occurring sedative and hallucinogen
Muscimol, also known as agarin, pantherine, or pyroibotenic acid, is a GABAA receptor agonist with sedative and hallucinogenic effects and the principal psychoactive
Muscimol
Sleep medication
modulator at the GABAA receptor. It is an imidazopyridine and increases GABA effects in the central nervous system by binding to GABAA receptors at the same
Zolpidem
17β-diol – GABAA receptor positive allosteric modulator 3α,5β-Androstanediol (etiocholanediol): 5β-androstane-3α,17β-diol – GABAA receptor positive allosteric
List_of_neurosteroids
Drug that blocks hallucinogen effects
also a GABAA receptor positive allosteric modulator with similar effects, has been used for such purposes as well. Besides serotonin 5-HT2A receptor antagonists
Trip_killer
Drug that induces convulsions
inverse agonists) at either the GABAA or/and glycine receptors (e.g the pesticide fipronil), or ionotropic glutamate receptor agonists (e.g the marine toxin
Convulsant
Intravenous medication used in anesthesia
actionsuggests potentiation of GABAA receptor activity by acting as a GABAA receptor positive allosteric modulator, which slows receptor channel-closing time.
Propofol
Compound that induces a loss of consciousness
mediate their effects: GABAA receptors are chloride channels that hyperpolarize neurons and function as inhibitory CNS receptors. General anesthetics that
General_anaesthetic
Chemical compound
hepatic encephalopathy. It acts as a negative allosteric modulator of the GABAA receptor. The medication selectively antagonizes the stimulatory actions of inhibitory
Golexanolone
Inhibitory neurotransmitter in the mammalian brain
classes of GABA receptor are known: GABAA in which the receptor is part of a ligand-gated ion channel complex GABAB metabotropic receptors, which are G protein-coupled
GABA
Chemical compound
former developmental code names Lu-2-030, MK-0928, and OV101, is a GABAA receptor agonist related to muscimol which was investigated for the treatment
Gaboxadol
amineptine, nomifensine) Serotonin 5-HT1A receptor agonists (e.g., gepirone, tandospirone) Neurosteroid-type GABAA receptor positive allosteric modulators (e
List of psychiatric drugs by type
List_of_psychiatric_drugs_by_type
Obsolete sedative–hypnotic drug
certain GABAA receptor subtypes, producing excitatory effects in neurons expressing those receptors. As such, methaqualone is considered a mixed GABAA receptor
Methaqualone
Protein-coding gene in humans
subunit forms specific GABAA receptor subtypes by co-assembly leading to δ subunit containing GABAA receptors (δ-GABAA receptors). The delta (δ) subunit,
GABRD
Short-acting barbiturate
barbiturates, pentobarbital binds to the barbiturate-binding site on the GABAA receptor. This action increases the duration of ion-channel opening. At high
Pentobarbital
Class of drugs
acid) – constituent of valerian; has anticonvulsant effects; PAM of the GABAA receptor Derivatives: isovalerate (isopentanoate/3-methylbutanoate), menthyl
GABA_analogue
Anxiolytic medication
Z-drug zolpidem, and acts as a GABAA receptor positive allosteric modulator of the benzodiazepine site of the receptor complex. In contrast to zolpidem
Alpidem
Pharmaceutical compound
biologically active, acting as a relatively potent GABAA receptor partial agonist and GABAA-ρ receptor antagonist or weak partial agonist. It shows varying
Imidazoleacetic_acid
Anticonvulsant medication
those of GABAA receptor agonists like gaboxadol and muscimol, primarily enhancing slow wave sleep, and differ from those of GABAA receptor positive allosteric
Tiagabine
Class of CNS depressant drugs
effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety)
Benzodiazepine
Pharmaceutical compound
4-PIOL, also known as 5-(4-piperidyl)isoxazol-3-ol, is a GABAA receptor agonist that was derived from THIP (gaboxadol). It is a non-ring-fused analogue
4-PIOL
Pharmaceutical compound
Dihydromuscimol (DHM), or 4,5-dihydromuscimol, is a synthetic GABAA receptor agonist and GABA reuptake inhibitor which was derived from the Amanita muscaria
Dihydromuscimol
Widely distributed inhibitory receptor in the central nervous system
dorsal root ganglion neurons despite the presence of GABAA receptors. Glycine and its receptor were first suggested to play a role in inhibition of cells
Glycine_receptor
Benzodiazepine sedative
positive allosteric modulators of the GABA type A receptors (GABAA). The GABAA receptors are ligand-gated chloride-selective ion channels that are activated
Diazepam
Pharmaceutical compound
Piperidine-4-sulfonic acid (P4S) is a synthetic GABAA receptor agonist and a cyclized analogue of the inhibitory neurotransmitter γ-aminobutyric acid (GABA)
Piperidine-4-sulfonic_acid
Investigational panic disorder drugs
STAP-001; UCB-7538) – GABAA receptor positive allosteric modulator and benzodiazepine [7] Alprazolam intranasal (Panistat) – GABAA receptor positive allosteric
List of investigational panic disorder drugs
List_of_investigational_panic_disorder_drugs
Chemical compound
phthalide-isoquinoline compound that is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and
Bicuculline
How drugs induce reversible suppression of consciousness
believed to be GABAA receptor, with particular β subunits playing a crucial role. The concept of specific interactions between receptors and drugs first
Theories of general anaesthetic action
Theories_of_general_anaesthetic_action
Protein molecule receiving signals for a cell
electrical activity of neurons by binding to GABAA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification
Receptor_(biochemistry)
Protein-coding gene in the species Homo sapiens
ionotropic GABAA receptors. GABA (γ-aminobutyric acid) system is the major inhibitory system in the brain, and its dominant GABAA receptor subtype is composed
GABRB2
Type of psychoactive fungus
contain the serotonin 5-HT2A receptor agonist psilocybin) and Amanita muscaria mushrooms (which contain the GABAA receptor agonist muscimol). Lanmaoa asiatica
Hallucinogenic bolete mushroom
Hallucinogenic_bolete_mushroom
Compounds that alter neuronal activity
neurotransmission. They act as positive allosteric modulators of the GABAA receptor (especially δ subunit-containing isoforms), and possess, in no particular
Neurosteroid
Benzodiazepine medication
neurotransmitter GABA at the GABAA receptor. Benzodiazepines, such as lorazepam, enhance the effects of GABA at the GABAA receptor via increasing the frequency
Lorazepam
Barbiturate general anesthetic
The GABAA receptor is an inhibitory channel that decreases neuronal activity, and barbiturates enhance the inhibitory action of the GABAA receptor. Following
Sodium_thiopental
Endogenous inhibitory neurosteroid
is a neurosteroid and acts as a positive allosteric modulator of the GABAA receptor, the major biological target of the inhibitory neurotransmitter γ-aminobutyric
Allopregnanolone
Pharmaceutical compound
is a low-potency GABAA receptor very weak partial agonist or antagonist related to gaboxadol (THIP). It is also a weak GABAA-ρ receptor antagonist and a
Thio-THIP
Class of depressant drugs derived from barbituric acid
GABAA receptor channel is only one of several representatives. This Cys-loop receptor superfamily of ion channels includes the neuronal nACh receptor
Barbiturate
Chemical compound
containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes
Bretazenil
Pharmaceutical compound
constrained derivative of γ-aminobutyric acid (GABA) and a moderately potent GABAA receptor partial agonist. It consists of a piperidine ring with a carboxylic
Isonipecotic_acid
Drug that binds to but does not activate muscarinic cholinergic receptors
A muscarinic acetylcholine receptor antagonist, also simply known as a muscarinic antagonist or as an antimuscarinic agent, is a type of anticholinergic
Muscarinic_antagonist
Pharmaceutical compound
potent GABAA-ρ receptor (GABAC receptor) antagonist related to gaboxadol (THIP). It is 4-fold more potent than gaboxadol as a GABAA-ρ receptor antagonist
Iso-THIP
Organic compound used as flavouring and analgesic
same sites on the GABAA receptor. Menthol may also enhance the activity of glycine receptors and negatively modulate 5-HT3 receptors and nAChRs. Menthol
Menthol
Benzodiazepine medication
benzodiazepine receptor partial agonist at the GABAA receptor and the effects are related to binding to one or more specific GABA receptor subunits, increasing
Clobazam
List of pharmaceutical drugs under clinical development for treatment of depression
GABAA receptor-preferring positive allosteric modulator and neurosteroid 4-Chlorokynurenine (4-CL-KYN; AV-101) – ionotropic glutamate NMDA receptor glycine
List of investigational antidepressants
List_of_investigational_antidepressants
Genetic disorder
function. GABRA5, GABRB3, and GABRG3 are gamma aminobutyric acid type A (GABAA) receptor subunit genes and are likely important in Dup15q syndrome given the
Dup15q
agonists (e.g., danavorexton, oveporexton) GABAA receptor agonists (e.g., muscimol, gaboxadol) GABAA receptor positive allosteric modulators Alcohols (e
List_of_psychoactive_drugs
Pharmaceutical compound
ENX-102, also known as TPA-023B, is a GABAA receptor positive allosteric modulator, nonbenzodiazepine, and investigational anxiolytic which is under development
ENX-102
Pharmaceutical compound
4-AHP, also known as 4-(aminomethyl)-1-hydroxypyrazole, is a synthetic GABAA receptor agonist related to the alkaloid and Amanita muscaria constituent muscimol
4-AHP
Class of psychoactive drugs
are similar in mechanism of action to benzodiazepine drugs, acting as GABAA receptor positive allosteric modulators of the benzodiazepine site, and therefore
Nonbenzodiazepine
Chemical compound
officinalis) and in M. grandiflora. Magnolol is a compound that acts on GABAA receptors and functions as an allosteric modulator. It has antifungal properties
Magnolol
Class of compounds
that contain this same chemical substructure. In general, they are GABAA receptor agonists, however recently proton pump inhibitors, aromatase inhibitors
Imidazopyridine
Class of analgesic drug
natural substances found in the opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects
Opioid
Benzodiazepine medication
during pregnancy may result in harm to the fetus. Clonazepam binds to GABAA receptors, thus increasing the effect of the chief inhibitory neurotransmitter
Clonazepam
Class of medications used to alleviate anxiety
GABAergic, NGF and BDNF release promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma receptor agonism thought to have some involvement. Bromantane
Anxiolytic
Pharmacodynamics and pharmacokinetics of ethanol
has been shown to affect ligand-gated ion channels, particularly the GABAA receptor. After oral ingestion, ethanol is absorbed via the stomach and intestines
Pharmacology_of_ethanol
Class of drugs
of one (selective orexin receptor antagonist, SORA) or both (dual orexin receptor antagonist, DORA) of the orexin receptors, OX1 and OX2. Medical applications
Orexin_antagonist
Chemical compound
GABAA receptors, with minimal functional activity at α1 subunit-containing GABAA receptors. A dose of darigabat that achieved more than 80% receptor occupancy
Darigabat
Hypnotic medication
positively modulates benzodiazepine-sensitive GABAA receptors and enhances GABA binding at the GABAA receptors to produce zopiclone's pharmacological properties
Zopiclone
Group of four possible stereoisomers found in various plants: a.o., absinthe and mint
psychoactive effects. Thujone acts on the GABAA receptor as an antagonist. As a competitive antagonist of GABAA receptor, thujone alone is considered to be convulsant
Thujone
Chemical compound
does not selectively label the GABRA1 subtype. GABAA receptor negative allosteric modulator GABAA receptor § Ligands Alcoholism US patent 4868176, Gardner
Ro15-4513
Class of drugs
diphenhydramine, and trihexyphenidyl κ-Opioid receptor agonists like salvinorin A, pentazocine, and levorphanol GABAA receptor agonists like muscimol and gaboxadol
Hallucinogen
GABA receptor antagonist drug and benzodiazepine antidote
Flumazenil, also known as flumazepil, is a selective GABAA receptor antagonist administered via injection, or intranasally. Therapeutically, it acts as
Flumazenil
Pharmaceutical compound
benzodiazepines are GABAA receptor positive allosteric modulators that act mainly upon γ2 subunit-containing GABAA receptors. GABAA receptor γ2 subunits are
NTX-1955
Chemical compound
inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive
Basmisanil
Medication
act as an NMDA receptor antagonist and positive allosteric modulator of GABAA receptors. The activity of acamprosate on those receptors is indirect, unlike
Acamprosate
Abandoned drug
MRK-409, also known as MK-0343, is a GABAA receptor partial agonist. It was designed to be a non-sedative anxiolytic, however its development was halted
MRK-409
and include: GABAA receptors GABAA-ρ receptors The GABAB receptor, a G protein-coupled receptor, is the only metabotropic GABA receptor and its mechanism
Ionotropic_GABA_receptor
Topics referred to by the same term
Gabaa may refer to: Gabâ, the concept of divine retribution in parts of the Philippines GABAA may refer to: GABAA receptor Gaaba, an Indian dish prepared
Gabaa
Drug class
Tiagabine (Gabitril) GABA transaminase inhibitor GABA receptor agonist GABAA receptor agonist GABAA receptor positive allosteric modulator Bauer J, Cooper-Mahkorn
GABA_reuptake_inhibitor
Polish neuroscientist
Her earlier work at the U.S. National Institute of Mental Health on GABAA receptor modulation by neurosteroid metabolites has been cited in later research
Maria_Dorota_Majewska
Investigational PMS/PMDD drugs
vomeropherine / "neurotransmitter receptor modulator" – PMDD [2] Sepranolone (isoallopregnanolone; UC-1010) – GABAA receptor negative allosteric modulator
List of investigational PMS/PMDD drugs
List_of_investigational_PMS/PMDD_drugs
for scientific research as model kappa opioid receptor agonists. In the mid-2010s, one mu opioid receptor selective compound from this class, U-47700,
Utopioid_(drug_class)
Class of cell surface receptors coupled to G-protein-associated intracellular signaling
protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G
G_protein-coupled_receptor
Chemical compound
TCS 1205 is a GABAA receptor positive allosteric modulator of the tryptamine family. It is a benzodiazepine site agonist selective for certain subunits
TCS-1205
Benzodiazepine sedative
such as alcohol and opioids. Flunitrazepam overdose responds to the GABAA receptor antagonist flumazenil, which thus can be used as a treatment. As of
Flunitrazepam
Chemical compound
in-vitro affinity to the picrotoxin binding site on the GABAA receptor. Many GABAA receptor ligands, such as diazepam and phenobarbital, are effective
Pentylenetetrazol
Substance that arouses sexual desires
receptor antagonists: Xanthines/methylxanthines Nicotine-type/nicotinic acetylcholine receptor agonists: Nicotine analogues Depressants GABAA receptor
Aphrodisiac
Pharmaceutical compound
5-aminomethyl-3-isothiazol, is a synthetic GABAA receptor agonist which is structurally related to the naturally occurring GABAA receptor agonist muscimol (found in Amanita
Thiomuscimol
Carbamate derivative used as an anxiolytic
system, including the thalamus and limbic system. Meprobamate binds to GABAA receptors which interrupts neuronal communication in the reticular formation
Meprobamate
Benzodiazepine medication
transmission to reduce anxiety. The GABAA receptor is made up of 5 subunits out of a possible 19, and GABAA receptors made up of different combinations
Alprazolam
G-protein coupled receptor
149184-22-5 SGS-742 GABA receptor GABAA receptor Hyland NP, Cryan JF (2010). "A Gut Feeling about GABA: Focus on GABA(B) Receptors". Frontiers in Pharmacology
GABAB_receptor
Species of plant
mitragynine and to a lesser extent, 7-hydroxymitragynine) that bind to opioid receptors, mostly as partial μ-opioid agonists. Kratom can also be subjectively
Mitragyna_speciosa
Chemical compound
Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would
Gabazine
Investigational PTSD drugs
Therapeutics (SAGE 105; SGE-202; SGE-301; SGE-516) – GABAA receptor modulators and NMDA receptor modulators [44] Research programme: psychedelic and empathogenic
List of investigational post-traumatic stress disorder drugs
List_of_investigational_post-traumatic_stress_disorder_drugs
(Valdoxan) – 5-HT2C receptor antagonist and MT1 and MT2 receptor agonist Brexanolone (allopregnanolone; Zulresso) – GABAA receptor positive allosteric
List_of_antidepressants
Chemical compound, anxiogenic
α3IA, also known as GTPL4094, is an inverse agonist of the GABAA receptor. It is more selective for the α3 subunit, hence its name. Agonism of the α3 subunit
Α3IA
Protein-coding gene in the species Homo sapiens
the gene codes for many protein isoforms, all being subunits in the GABAA receptor, a ligand-gated ion channel. The beta-3 subunit is expressed at different
GABRB3
Chemical compound
potent GABAA receptor positive allosteric modulators, and hence interactions with the TSPO can also indirectly potentiate the GABAA receptor. The precise
Deuterated_etifoxine
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GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
GABAA RECEPTOR
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