GABA Agonists

Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
DrugDrug NameDrug Indication
DB00181BaclofenBaclofen is administered for the relief of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and associated pain and clonus, in addition to muscular rigidity [FDA label]. Patients receiving this drug should have reversible spasticity for baclofen to promote the restoration of residual function. This drug is not indicated in the treatment of skeletal muscle spasm caused by rheumatic disorders. The efficacy of baclofen in stroke, cerebral palsy, and Parkinson's disease has not been determined and, therefore, baclofen is not recommended for these conditions [FDA label].
DB00425ZolpidemThis drug is indicated for the short-term treatment of insomnia in adults characterized by difficulties with sleep initiation [FDA label].
DB00837ProgabideIndicated for the treatment of epilepsy.
DB00906TiagabineFor the treatment of partial seizures
DB05404AZD 3355Investigated for use/treatment in gastroesophageal reflux disease (GERD).
DB06527TramiprosateInvestigated for use/treatment in strokes and alzheimer's disease.
DB06554GaboxadolInvestigated for use/treatment in sleep disorders and insomnia.
DB06579AdipiplonInvestigated for use/treatment in insomnia and sleep disorders.
DB08892Arbaclofen PlacarbilInvestigated for the treatment of spasticity in multiple sclerosis, acute back spasms, and GERD.
DB11920LesogaberanNot Available
DB12458MuscimolNot Available
DB13455PhenibutNot Available
DB00962ZaleplonFor the treatment of short-term treatment of insomnia in adults.
DrugDrug NameTargetType
DB00181BaclofenGamma-aminobutyric acid type B receptor subunit 1target
DB00181BaclofenGamma-aminobutyric acid type B receptor subunit 2target
DB00425ZolpidemGamma-aminobutyric acid receptor subunit alpha-1target
DB00425ZolpidemCytochrome P450 3A4enzyme
DB00425ZolpidemCytochrome P450 1A2enzyme
DB00425ZolpidemGamma-aminobutyric acid receptor subunit alpha-2target
DB00425ZolpidemGamma-aminobutyric acid receptor subunit alpha-3target
DB00425ZolpidemCytochrome P450 2C9enzyme
DB00425ZolpidemCytochrome P450 2C19enzyme
DB00425ZolpidemCytochrome P450 2D6enzyme
DB00425ZolpidemGamma-aminobutyric acid receptor subunit gamma-2target
DB00837ProgabideGamma-aminobutyric acid receptor subunit alpha-1target
DB00837ProgabideGamma-aminobutyric acid type B receptor subunit 1target
DB00906TiagabineSodium- and chloride-dependent GABA transporter 1target
DB00906TiagabineCytochrome P450 3A4enzyme
DB00906TiagabineUDP-glucuronosyltransferase 1-1enzyme
DB05404AZD 3355Cellular tumor antigen p53target
DB06554GaboxadolProton-coupled amino acid transporter 1transporter
DB06579AdipiplonGABA-A receptor (benzodiazepine site)target
DB08892Arbaclofen PlacarbilMonocarboxylate transporter 1transporter
DB08892Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 1target
DB08892Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 2target
DB12458MuscimolGamma-aminobutyric acid receptor subunit alpha-1target
DB12458MuscimolGamma-aminobutyric acid receptor subunit beta-3target
DB12458MuscimolGamma-aminobutyric acid receptor subunit gamma-2target
DB00962ZaleplonTranslocator proteintarget
DB00962ZaleplonGamma-aminobutyric acid receptor subunit alpha-1target
DB00962ZaleplonCytochrome P450 3A4enzyme
DB00962ZaleplonAldehyde oxidaseenzyme
DB00962ZaleplonCytochrome P450 3A5enzyme
DB00962ZaleplonCytochrome P450 3A7enzyme