GABA Modulators

GABA Modulators
Accession Number

Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.

DrugDrug Description
LorazepamA long-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and seizures.
TemazepamA short-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and insomnia.
PentobarbitalA barbiturate drug used to induce sleep, cause sedation, and control certain types of seizures.
AlprazolamA long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders and generalized anxiety in addition to anxiety associated with depression.
SecobarbitalA barbiturate used for the short-term treatment of insomnia.
ChlordiazepoxideA benzodiazepine used to treat the withdrawal symptoms of acute alcoholism, to treat preoperative anxiety, and to treat anxiety over a short term period.
ThiopentalA barbiturate used to induce general anesthesia, treat convulsions, and reduce intracranial pressure.
Clorazepic acidA benzodiazepine used to treat anxiety, partial seizures, and alcohol withdrawal.
MidazolamA short-acting injectable benzodiazepine with rapid onset that is commonly used in seizures, anesthesia and anxiety disorders.
FlurazepamA long-acting benzodiazepine with a rapid onset of action that is commonly used to treat insomnia.
DiazepamA long-acting benzodiazepine with rapid onset commonly used to treat panic disorders, severe anxiety, alcohol withdrawal, and seizures.
OxazepamAn intermediate-acting benzodiazepine with slow onset commonly used to treat panic disorders, severe anxiety, alcohol withdrawals, and insomnia.
MethylphenobarbitalFor the relief of anxiety, tension, and apprehension, also used as an anticonvulsant for the treatment of epilepsy.
TriazolamA benzodiazepine used for short term treatment of insomnia.
ZaleplonA sedative used for short term treatment of insomnia in adults.
ClonazepamA long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders, severe anxiety, and seizures.
ThiamylalUsed for the production of complete anaesthesia of short duration, for the induction of general anaesthesia, and for inducing a hypnotic state.
PhenobarbitalA long-lasting barbiturate and anticonvulsant used in the treatment of all types of seizures, except for absent seizures.
FlumazenilA benzodiazepine antagonist that is used for the complete or partial reversal of the sedative effects caused by benzodiazepines in various clinical settings, such as induced general anesthesia for diagnostic and therapeutic procedures.
EstazolamA benzodiazepine used for the short-term management of insomnia.
AmobarbitalA barbiturate derivative used for the induction of sedation during procedures, short-term management of insomnia, and acute management of refractory tonic-clonic seizures.
HexobarbitalFor the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful...
BarbitalA long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice...
FlunitrazepamFor short-term treatment of severe insomnias, that are not responsive to other hypnotics.
BromazepamA short-acting benzodiazepine with intermediate onset commonly used to treat panic disorders and severe anxiety.
PrazepamFor the treatment of anxiety disorders.
NitrazepamA long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders, severe anxiety, insomnia, and seizures.
ClomethiazoleInvestigated for use/treatment in strokes.
ZolazepamZolazepam is a pyrazolodiazepinone derivative used as an anaesthetic in veterinary medicine. Zolazepam is typically used in combination with the NMDA antagonist tiletamine or the α2 adrenoceptor agonist xylazine. It...
IndiplonIndiplon has been used in trials studying the treatment of Insomnia and Depression.
MedazepamNot Annotated
AZD-7325AZD7325 is a high affinity, selective modulator of the GABAA receptor system.
NordazepamAn intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.
BrexanoloneBrexanolone is a synthetic neuroactive steroid gamma-aminobutyric acid A (GABA(a)) receptor positive modulator indicated for the treatment of postpartum depression (PPD) in adult women [FDA Label][A176080, A176083, F4063, F4066, F4072].
PrimidoneAn antiepileptic used to treat grand mal, psychomotor, and focal epileptic seizures.
PyrazolamNot Annotated
CenobamateA small molecule drug indicated to treat partial onset seizures in adults.
RemimazolamAn ultra short-acting benzodiazepine used for the induction and maintenence of procedural sedation during short procedures.
Drugs & Drug Targets
LorazepamUDP-glucuronosyltransferase 2B15enzyme
LorazepamGABA(A) Receptortarget
LorazepamCytochrome P450 3A4enzyme
LorazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
TemazepamCytochrome P450 3A4enzyme
TemazepamCytochrome P450 2B6enzyme
TemazepamCytochrome P450 2C9enzyme
TemazepamGABA(A) Receptortarget
TemazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
PentobarbitalCytochrome P450 3A4enzyme
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-4target
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-6target
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-2target
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-3target
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-5target
PentobarbitalNeuronal acetylcholine receptor subunit alpha-4target
PentobarbitalNeuronal acetylcholine receptor subunit alpha-7target
PentobarbitalGlutamate receptor 2target
PentobarbitalGlutamate receptor ionotropic, kainate 2target
PentobarbitalCytochrome P450 2C19enzyme
PentobarbitalCytochrome P450 2A6enzyme
PentobarbitalGABA(A) Receptortarget
PentobarbitalNMDA receptortarget
PentobarbitalNuclear receptor subfamily 1 group I member 2target
AlprazolamCytochrome P450 3A4enzyme
AlprazolamCytochrome P450 2C9enzyme
AlprazolamCytochrome P450 3A5enzyme
AlprazolamCytochrome P450 3A7enzyme
AlprazolamGABA(A) Receptortarget
AlprazolamSerum albumincarrier
Alprazolamalpha1-acid glycoproteincarrier
AlprazolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
SecobarbitalCytochrome P450 2C8enzyme
SecobarbitalCytochrome P450 2C9enzyme
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-2target
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-3target
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-4target
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-5target
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-6target
SecobarbitalNeuronal acetylcholine receptor subunit alpha-4target
SecobarbitalNeuronal acetylcholine receptor subunit alpha-7target
SecobarbitalGlutamate receptor 2target
SecobarbitalGlutamate receptor ionotropic, kainate 2target
SecobarbitalCytochrome P450 1A2enzyme
SecobarbitalNMDA receptortarget
SecobarbitalCytochrome P450 2C19enzyme
ChlordiazepoxideGABA(A) Receptortarget
ChlordiazepoxideGABA(A) Receptor Benzodiazepine Binding Sitetarget
ThiopentalGamma-aminobutyric acid receptor subunit alpha-1target
ThiopentalFatty-acid amide hydrolase 1target
ThiopentalGamma-aminobutyric acid receptor subunit alpha-2target
ThiopentalGamma-aminobutyric acid receptor subunit alpha-3target
ThiopentalGamma-aminobutyric acid receptor subunit alpha-4target
ThiopentalGamma-aminobutyric acid receptor subunit alpha-5target
ThiopentalGamma-aminobutyric acid receptor subunit alpha-6target
ThiopentalNeuronal acetylcholine receptor subunit alpha-4target
ThiopentalNeuronal acetylcholine receptor subunit alpha-7target
ThiopentalGlutamate receptor 2target
ThiopentalGlutamate receptor ionotropic, kainate 2target
ThiopentalCytochrome P450 3A Subfamilyenzyme
ThiopentalMuscarinic acetylcholine receptor M3target
ThiopentalCytochrome P450 2C19enzyme
Clorazepic acidCytochrome P450 3A4enzyme
Clorazepic acidGABA(A) Receptortarget
Clorazepic acidGABA(A) Receptor Benzodiazepine Binding Sitetarget
MidazolamCytochrome P450 3A4enzyme
MidazolamCytochrome P450 3A5enzyme
MidazolamUDP-glucuronosyltransferase 1-4enzyme
MidazolamCytochrome P450 3A7enzyme
MidazolamGABA(A) Receptortarget
MidazolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
FlurazepamCytochrome P450 3A4enzyme
FlurazepamP-glycoprotein 1transporter
FlurazepamCytochrome P450 2E1enzyme
FlurazepamCytochrome P450 2A6enzyme
FlurazepamSolute carrier family 22 member 2transporter
FlurazepamGABA(A) Receptortarget
FlurazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
DiazepamCytochrome P450 3A4enzyme
DiazepamSerum albumincarrier
DiazepamCytochrome P450 2C9enzyme
DiazepamCytochrome P450 2C19enzyme
DiazepamCytochrome P450 3A5enzyme
DiazepamCytochrome P450 3A7enzyme
DiazepamP-glycoprotein 1transporter
DiazepamCytochrome P450 2B6enzyme
DiazepamProstaglandin G/H synthase 1enzyme
DiazepamCytochrome P450 2C18enzyme
DiazepamCytochrome P450 2C8enzyme
DiazepamCytochrome P450 2E1enzyme
DiazepamGABA(A) Receptortarget
DiazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
OxazepamUDP-glucuronosyltransferase 2B15enzyme
OxazepamUDP-glucuronosyltransferase 2B7enzyme
OxazepamUDP-glucuronosyltransferase 1-9enzyme
OxazepamGABA(A) Receptortarget
OxazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
OxazepamSerum albumincarrier
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
MethylphenobarbitalCytochrome P450 2C19enzyme
MethylphenobarbitalCytochrome P450 2B6enzyme
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-2target
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-3target
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-4target
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-5target
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-6target
MethylphenobarbitalNeuronal acetylcholine receptor subunit alpha-4target
MethylphenobarbitalNeuronal acetylcholine receptor subunit alpha-7target
MethylphenobarbitalGlutamate receptor 2target
MethylphenobarbitalGlutamate receptor ionotropic, kainate 2target
MethylphenobarbitalNuclear receptor subfamily 1 group I member 2target
TriazolamCytochrome P450 3A4enzyme
TriazolamCytochrome P450 3A5enzyme
TriazolamCytochrome P450 3A7enzyme
TriazolamCytochrome P450 2C8enzyme
TriazolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
TriazolamGABA(A) Receptortarget
ZaleplonGamma-aminobutyric acid receptor subunit alpha-1target
ZaleplonCytochrome P450 3A4enzyme
ZaleplonAldehyde oxidaseenzyme
ZaleplonCytochrome P450 3A5enzyme
ZaleplonCytochrome P450 3A7enzyme
ClonazepamCytochrome P450 3A4enzyme
ClonazepamSerum albumincarrier
ClonazepamCytochrome P450 2E1enzyme
ClonazepamArylamine N-acetyltransferase 2enzyme
ClonazepamGABA(A) Receptortarget
ClonazepamNuclear receptor subfamily 1 group I member 2target
ClonazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
ThiamylalGamma-aminobutyric acid receptor subunit alpha-1target
ThiamylalATP-sensitive inward rectifier potassium channel 8target
ThiamylalATP-sensitive inward rectifier potassium channel 11target
ThiamylalCytochrome P450 2C9enzyme
ThiamylalCytochrome P450 3A4enzyme
ThiamylalCytochrome P450 2E1enzyme
PhenobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
PhenobarbitalCytochrome P450 2C19enzyme
PhenobarbitalCytochrome P450 2C9enzyme
PhenobarbitalCytochrome P450 2B6enzyme
PhenobarbitalCytochrome P450 2C8enzyme
PhenobarbitalCytochrome P450 1A2enzyme
PhenobarbitalCytochrome P450 3A4enzyme
PhenobarbitalCanalicular multispecific organic anion transporter 2transporter
PhenobarbitalBile salt export pumptransporter
PhenobarbitalP-glycoprotein 1transporter
PhenobarbitalMultidrug resistance-associated protein 1transporter
PhenobarbitalSolute carrier organic anion transporter family member 2A1transporter
PhenobarbitalCanalicular multispecific organic anion transporter 1transporter
PhenobarbitalNeuronal acetylcholine receptor subunit alpha-4target
PhenobarbitalNeuronal acetylcholine receptor subunit alpha-7target
PhenobarbitalGlutamate receptor 2target
PhenobarbitalGlutamate receptor ionotropic, kainate 2target
PhenobarbitalCytochrome P450 2A6enzyme
PhenobarbitalCytochrome P450 2E1enzyme
PhenobarbitalCytochrome P450 3A5enzyme
PhenobarbitalCytochrome P450 1A1enzyme
PhenobarbitalCytochrome P450 2C18enzyme
PhenobarbitalCytochrome P450 3A7enzyme
PhenobarbitalCytochrome P450 4B1enzyme
PhenobarbitalNMDA receptortarget
PhenobarbitalNuclear receptor subfamily 1 group I member 2target
PhenobarbitalUDP-glucuronosyltransferase 1-1enzyme
PhenobarbitalUDP-glucuronosyltransferase 2B7enzyme
FlumazenilGamma-aminobutyric acid receptor subunit alpha-1target
FlumazenilGamma-aminobutyric acid receptor subunit gamma-2target
FlumazenilGamma-aminobutyric acid receptor subunit alpha-5target
FlumazenilGABA(A) Receptortarget
EstazolamCytochrome P450 3A4enzyme
EstazolamGABA(A) Receptortarget
EstazolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-4target
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-6target
AmobarbitalNeuronal acetylcholine receptor subunit alpha-4target
AmobarbitalNeuronal acetylcholine receptor subunit alpha-7target
AmobarbitalGlutamate receptor 2target
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-2target
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-3target
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-5target
AmobarbitalGlutamate receptor ionotropic, kainate 2target
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
HexobarbitalCytochrome P450 2C9enzyme
HexobarbitalCytochrome P450 2C19enzyme
HexobarbitalProstaglandin G/H synthase 1enzyme
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-2target
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-3target
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-4target
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-5target
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-6target
HexobarbitalNeuronal acetylcholine receptor subunit alpha-4target
HexobarbitalNeuronal acetylcholine receptor subunit alpha-7target
HexobarbitalGlutamate receptor 2target
HexobarbitalGlutamate receptor ionotropic, kainate 2target
BarbitalGamma-aminobutyric acid receptor subunit alpha-1target
BarbitalGamma-aminobutyric acid receptor subunit alpha-2target
BarbitalGamma-aminobutyric acid receptor subunit alpha-3target
BarbitalGamma-aminobutyric acid receptor subunit alpha-4target
BarbitalGamma-aminobutyric acid receptor subunit alpha-5target
BarbitalGamma-aminobutyric acid receptor subunit alpha-6target
BarbitalNeuronal acetylcholine receptor subunit alpha-4target
BarbitalNeuronal acetylcholine receptor subunit alpha-7target
BarbitalGlutamate receptor 2target
BarbitalGlutamate receptor ionotropic, kainate 2target
BarbitalCytochrome P450 3A4enzyme
BarbitalCytochrome P450 2C19enzyme
FlunitrazepamCytochrome P450 2C19enzyme
FlunitrazepamUDP-glucuronosyltransferase 2B7enzyme
FlunitrazepamCytochrome P450 2A6enzyme
FlunitrazepamCytochrome P450 2B6enzyme
FlunitrazepamCytochrome P450 2C9enzyme
FlunitrazepamCytochrome P450 3A4enzyme
FlunitrazepamCytochrome P450 2E1enzyme
FlunitrazepamUDP-glucuronosyltransferase 1-1enzyme
FlunitrazepamUDP-glucuronosyltransferase 1-3enzyme
FlunitrazepamGABA(A) Receptortarget
FlunitrazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
BromazepamCytochrome P450 1A2enzyme
BromazepamCytochrome P450 2C19enzyme
BromazepamCytochrome P450 2E1enzyme
BromazepamGABA(A) Receptortarget
BromazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
PrazepamCytochrome P450 3A4enzyme
PrazepamGABA(A) Receptortarget
PrazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
NitrazepamSodium channel protein type 1 subunit alphatarget
NitrazepamCytochrome P450 3A4enzyme
NitrazepamCytochrome P450 2E1enzyme
NitrazepamGABA(A) Receptortarget
NitrazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
ClomethiazoleGamma-aminobutyric acid receptor subunit alpha-1target
ClomethiazoleCytochrome P450 2A6enzyme
ClomethiazoleCytochrome P450 2B6enzyme
ClomethiazoleCytochrome P450 2C19enzyme
ClomethiazoleCytochrome P450 3A4enzyme
MedazepamGABA(A) Receptortarget
MedazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
AZD-7325Gamma-aminobutyric acid receptor subunit alpha-3target
AZD-7325Gamma-aminobutyric acid receptor subunit alpha-2target
NordazepamGABA(A) Receptortarget
NordazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
BrexanoloneGABA(A) Receptortarget
BrexanoloneAldose reductaseenzyme
PrimidoneGamma-aminobutyric acid receptor subunit alpha-1target
PrimidoneCytochrome P450 2C19enzyme
PrimidoneCytochrome P450 2C9enzyme
PrimidoneCytochrome P450 3A4enzyme
PrimidoneGamma-aminobutyric acid receptor subunit alpha-2target
PrimidoneGamma-aminobutyric acid receptor subunit alpha-3target
PrimidoneGamma-aminobutyric acid receptor subunit alpha-4target
PrimidoneGamma-aminobutyric acid receptor subunit alpha-5target
PrimidoneGamma-aminobutyric acid receptor subunit alpha-6target
PrimidoneNeuronal acetylcholine receptor subunit alpha-4target
PrimidoneNeuronal acetylcholine receptor subunit alpha-7target
PrimidoneGlutamate receptor 2target
PrimidoneGlutamate receptor ionotropic, kainate 2target
PrimidoneGABA(A) Receptortarget
PrimidoneTransient receptor potential cation channel subfamily M member 3transporter
PrimidoneCytochrome P450 2E1enzyme
PrimidoneCytochrome P450 1A2enzyme
PrimidoneUDP-glucuronosyltransferases (UGTs)enzyme
CenobamateUDP-glucuronosyltransferase 2B7enzyme
CenobamateUDP-glucuronosyltransferase 2B4enzyme
CenobamateCytochrome P450 2E1enzyme
CenobamateCytochrome P450 2A6enzyme
CenobamateCytochrome P450 2B6enzyme
CenobamateCytochrome P450 2C19enzyme
CenobamateCytochrome P450 3A4enzyme
CenobamateCytochrome P450 3A5enzyme
CenobamateSerum albumincarrier
CenobamateCytochrome P450 2C8enzyme
RemimazolamLiver carboxylesterase 1enzyme
RemimazolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
RemimazolamGABA(A) Receptortarget
RemimazolamSerum albumincarrier