GABA-A receptor — Drug Target
All drugs that target GABA-A receptor — marketed and clinical-stage. Includes 24 drug classes acting on this target.
Drug classes
GABA-A receptor agonist / General anesthetic · Intravenous anesthetic combination · Benzodiazepine · Intravenous sedative-hypnotic · Intravenous anesthetic · Sedative-hypnotic · Barbiturate · fospropofol · Benzodiazepine (topical) + sham procedure · GABA-A receptor positive allosteric modulator · Sedative-hypnotic, intravenous anesthetic · Benzodiazepine + propofol combination sedative-hypnotic
Marketed (61)
- total intravenous anesthetics · Università Vita-Salute San Raffaele · GABA-A receptor agonist / General anesthetic · Anesthesiology
Total intravenous anesthetics are a class of drugs that induce and maintain general anesthesia by depressing the central nervous system through enhancement of GABAergic inhibitory neurotransmission. - Sedation Etomidate combined with propofol · RenJi Hospital · Intravenous anesthetic combination · Anesthesia
A combination of two intravenous anesthetic agents that work synergistically to produce rapid sedation and hypnosis through GABAergic and other central nervous system pathways. - Diazepam Tablets · Queen Sirikit National Institute of Child Health · Benzodiazepine · Neurology, Psychiatry
Diazepam enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, reducing neuronal excitability. - total intravenous anaesthesia with Propofol. · Centre Hospitalier Universitaire Dijon · Intravenous sedative-hypnotic · Anesthesiology
Propofol is a rapid-acting intravenous sedative-hypnotic that enhances inhibitory GABA neurotransmission in the central nervous system to produce unconsciousness and anesthesia. - Midazolam (sedative) · Technische Universität Dresden · Benzodiazepine · Neurology / Anesthesia
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation and anxiolysis. - Group C : Saline + propofol group · Seoul National University Hospital · Intravenous anesthetic · Anesthesiology
Propofol is an intravenous anesthetic that enhances inhibitory GABA neurotransmission in the central nervous system, while saline serves as a vehicle for administration. - Alprazolam (Xanax) · University of California, San Diego · Benzodiazepine · Psychiatry/Neurology
Alprazolam enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, reducing neuronal excitability and producing anxiolytic and sedative effects. - (alprax) alprazolam · B.P. Koirala Institute of Health Sciences · Benzodiazepine · Psychiatry/Neurology
Alprazolam enhances the inhibitory effects of GABA at the GABA-A receptor in the central nervous system, reducing neuronal excitability and producing anxiolytic and sedative effects. - Sedation Propofol · RenJi Hospital · Intravenous sedative-hypnotic · Anesthesia/Sedation
Propofol is a rapid-acting intravenous sedative-hypnotic that enhances inhibitory GABA neurotransmission in the central nervous system. - propofol injectable emulsion · Life Extension Foundation Inc. · Sedative-hypnotic · Anesthesia
Propofol is a sedative-hypnotic agent that enhances inhibitory GABA neurotransmission in the central nervous system to produce rapid unconsciousness and sedation. - Valtoco Nasal Product · University Hospitals Cleveland Medical Center · Benzodiazepine · Neurology
Valtoco is a nasal spray formulation of diazepam that rapidly delivers the benzodiazepine to the systemic circulation to provide fast-acting seizure relief. - Midazolam Mylan · Universitaire Ziekenhuizen KU Leuven · Benzodiazepine · Central Nervous System / Anesthesia
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation, anxiolysis, and muscle relaxation. - midazolam in children premedication · Azienda Ospedaliera Universitaria Policlinico "G. Martino" · Benzodiazepine · Anesthesia/Sedation
Midazolam is a benzodiazepine that enhances inhibitory GABAergic neurotransmission in the central nervous system to produce sedation and anxiolysis. - Rematazolam Besylate · Second Affiliated Hospital of Nanchang University · Benzodiazepine · Neurology / Anesthesia
Rematazolam besylate is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors in the central nervous system. - remimazolam group · Gangnam Severance Hospital · Benzodiazepine · Anesthesia/Sedation
Remimazolam is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors, producing sedation and anxiolysis. - Remimazolam Tosilate for Injection · Jiangsu HengRui Medicine Co., Ltd. · Benzodiazepine · Anesthesia/Sedation
Remimazolam is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors, producing sedation and anxiolysis. - Phenobarbital Sodium Injection · PharPoint Research, Inc. · Barbiturate · Neurology
Phenobarbital sodium is a barbiturate that enhances inhibitory GABA neurotransmission in the central nervous system, producing sedative, hypnotic, and anticonvulsant effects. - Midazolam load · University of Pennsylvania · Benzodiazepine · Anesthesia, Sedation, Anxiety
Midazolam is a benzodiazepine that enhances inhibitory GABA neurotransmission in the central nervous system to produce sedation, anxiolysis, and amnesia. - midazolam intravenous administration · University Hospital, Lille · Benzodiazepine · Anesthesia/Sedation
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation, anxiolysis, and amnesia. - nasal diazepam · University of Cincinnati · Benzodiazepine · Neurology; Psychiatry
Nasal diazepam is a benzodiazepine that enhances inhibitory GABAergic neurotransmission in the central nervous system when administered intranasally. - Lusedra · fospropofol · Neuroscience
- Oral alprazolam · Isfahan University of Medical Sciences · Benzodiazepine · Psychiatry/Neurology
Alprazolam enhances the inhibitory effects of GABA at the GABA-A receptor, reducing neuronal excitability and producing anxiolytic and sedative effects. - Oral chloral hydrate · Seoul National University Hospital · Sedative-hypnotic · Neurology / Sleep Medicine
Chloral hydrate is a sedative-hypnotic that enhances inhibitory neurotransmission in the central nervous system, primarily through potentiation of GABA receptors. - Continuous Infusion Remimazolam · Second Affiliated Hospital of Wenzhou Medical University · Benzodiazepine · Anesthesia/Sedation
Remimazolam is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors, producing sedation and anxiolysis. - Sham laser plus topical clonazepam · Universidad Nacional Autonoma de Mexico · Benzodiazepine (topical) + sham procedure · Psychiatry / Pain Management / Dermatology
Sham laser plus topical clonazepam combines a placebo laser procedure with a benzodiazepine applied to the skin to reduce anxiety and pain symptoms. - lipuro propofol · Institute of Child Health · GABA-A receptor positive allosteric modulator · Anesthesia
Lipuro propofol is a lipid emulsion formulation of propofol that acts as a positive allosteric modulator of GABA-A receptors to produce sedation and anesthesia. - lorazepam (Ativan) · National Institute on Alcohol Abuse and Alcoholism (NIAAA) · Benzodiazepine · Psychiatry, Neurology
Lorazepam enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, reducing neuronal excitability. - Lorazepam (drug) · University of Manitoba · Benzodiazepine · Psychiatry, Neurology
Lorazepam enhances the inhibitory effects of GABA at the GABA-A receptor, reducing neuronal excitability and producing sedative, anxiolytic, and anticonvulsant effects. - Propofol (Group P) · All India Institute of Medical Sciences · Sedative-hypnotic, intravenous anesthetic · Anesthesia
Propofol is a sedative-hypnotic agent that enhances inhibitory GABA neurotransmission in the central nervous system, leading to rapid onset of unconsciousness. - Remimazolam besylate + propofol MCT · Chung-Ang University Gwangmyeong Hospital · Benzodiazepine + propofol combination sedative-hypnotic · Anesthesia/Sedation
Remimazolam besylate is a benzodiazepine that enhances GABAergic inhibition in the central nervous system, while propofol MCT is a lipophilic sedative-hypnotic that potentiates GABA receptor activity; together they provide rapid-onset, short-acting sedation and anesthesia. - Midazolam (active placebo) · Taipei Veterans General Hospital, Taiwan · Benzodiazepine · Neurology; Anesthesia; Psychiatry
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation and anxiolysis. - Ativan® · University of South Florida · Benzodiazepine · Psychiatry/Neurology
Ativan (lorazepam) enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, reducing neuronal excitability. - Manual titration of propofol · Brugmann University Hospital · Intravenous sedative-hypnotic · Anesthesia
Propofol is an intravenous sedative-hypnotic agent that enhances inhibitory GABAergic neurotransmission in the central nervous system to produce sedation and anesthesia. - Propofol Injection · Second Affiliated Hospital, School of Medicine, Zhejiang University · Intravenous sedative-hypnotic · Anesthesia
Propofol is a rapid-acting intravenous sedative-hypnotic agent that enhances inhibitory GABA neurotransmission in the central nervous system. - Propofol based general anesthesia · The First Affiliated Hospital of Anhui Medical University · Sedative-hypnotic; GABA-A receptor positive allosteric modulator · Anesthesiology
Propofol is a sedative-hypnotic agent that enhances inhibitory GABA neurotransmission in the central nervous system to produce rapid unconsciousness and anesthesia. - Propofol MCT · Chung-Ang University Gwangmyeong Hospital · General anesthetic · Anesthesia
Propofol MCT is a medium-chain triglyceride formulation of propofol that acts as a positive allosteric modulator of GABA-A receptors to produce rapid sedation and anesthesia. - Sevoflurane+Propofol · Huazhong University of Science and Technology · General anesthetic combination · Anesthesiology
Sevoflurane and propofol are combined inhalational and intravenous anesthetics that enhance GABAergic inhibitory neurotransmission to produce sedation, hypnosis, and anesthesia. - Midazolam sedation · University of Liege · Benzodiazepine · Anesthesia/Sedation
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation and anxiolysis. - Remimazolam based total intravenous anesthesia · The First Affiliated Hospital of Anhui Medical University · Benzodiazepine · Anesthesia
Remimazolam is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors, producing sedation and anesthesia. - Lorazepam and fMRI · University of Michigan · Benzodiazepine · Neurology; Psychiatry
Lorazepam is a benzodiazepine that enhances GABAergic inhibitory neurotransmission in the central nervous system, and fMRI is a neuroimaging technique used to visualize brain activity changes in response to the drug.
Phase 3 pipeline (22)
- Anesthesia induction with propofol · Daegu Catholic University Medical Center · GABA-A receptor positive allosteric modulator · Anesthesiology
Propofol is a rapid-acting intravenous anesthetic that enhances inhibitory GABA-A receptor signaling in the central nervous system to produce sedation and unconsciousness. - Etomidate Injectable Emulsion · Hunan Kelun Pharmaceutical Co., Ltd. · GABA-A receptor positive allosteric modulator; general anesthetic · Anesthesiology
Etomidate is a rapid-acting intravenous anesthetic that enhances GABAergic inhibitory neurotransmission in the central nervous system. - Eszopiclone 3 mg- Non-elderly · Eisai Co., Ltd. · Nonbenzodiazepine hypnotic (Z-drug) · Neurology / Sleep Medicine
Eszopiclone is a nonbenzodiazepine hypnotic that binds to GABA-A receptors in the brain to enhance inhibitory neurotransmission and promote sleep. - DZP · UCB Biopharma SRL · Benzodiazepine · Neurology, Psychiatry
DZP is a benzodiazepine that enhances GABAergic neurotransmission by potentiating the effect of GABA at GABA-A receptors in the central nervous system. - Eszopiclone 2 mg- Non-elderly · Eisai Co., Ltd. · Nonbenzodiazepine hypnotic (Z-drug) · Neurology / Sleep Medicine
Eszopiclone is a nonbenzodiazepine hypnotic that binds to GABA-A receptors in the brain to enhance inhibitory neurotransmission and promote sleep. - Eszopiclone 1 mg- Elderly · Eisai Co., Ltd. · Nonbenzodiazepine hypnotic (Z-drug) · Neurology / Sleep Medicine
Eszopiclone is a nonbenzodiazepine hypnotic that binds to GABA-A receptors in the brain to promote sleep onset and maintenance. - ICI35,868 (Diprivan) · AstraZeneca · Intravenous sedative-hypnotic · Anesthesia
Propofol is a rapid-acting intravenous sedative-hypnotic agent that enhances inhibitory GABAergic neurotransmission in the central nervous system. - Midazolam HCI · Eisai Inc. · Benzodiazepine · Neurology/Anesthesia
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation, anxiolysis, and muscle relaxation. - Extended-release lorazepam · Edgemont Pharmaceuticals, LLC · Benzodiazepine · Psychiatry / Neurology
Extended-release lorazepam is a benzodiazepine that enhances the inhibitory neurotransmitter GABA at the GABA-A receptor, producing anxiolytic, sedative, and anticonvulsant effects. - The midazolam group · Kasr El Aini Hospital · Benzodiazepine · Anesthesia, Sedation, Anxiety
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at the GABA-A receptor, producing sedation, anxiolysis, and muscle relaxation. - Clobazam Medium Dose · Lundbeck LLC · Benzodiazepine · Neurology
Clobazam is a benzodiazepine that enhances inhibitory GABAergic neurotransmission in the central nervous system to reduce seizure activity. - Clobazam High Dose · Lundbeck LLC · Benzodiazepine · Neurology
Clobazam is a benzodiazepine that enhances inhibitory GABAergic neurotransmission in the central nervous system to reduce seizure activity. - Midazolam oral intake · Hospices Civils de Lyon · Benzodiazepine · Psychiatry/Neurology
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at GABA-A receptors in the central nervous system, producing sedation and anxiolysis. - NRL-1 · Neurelis, Inc. · Neuroactive steroid; GABA-A receptor positive allosteric modulator · Neurology
NRL-1 is a neuroactive steroid that enhances GABAergic inhibitory neurotransmission in the central nervous system. - Anesthesia induction with remimazolam · Daegu Catholic University Medical Center · Benzodiazepine · Anesthesiology
Remimazolam is a benzodiazepine that enhances GABAergic neurotransmission by binding to GABA-A receptors, producing rapid sedation and anesthesia induction. - Staccato alprazolam · UCB Biopharma SRL · Benzodiazepine · Psychiatry / Neurology
Staccato alprazolam is a rapidly-absorbed inhaled formulation of alprazolam that binds to GABA-A receptors in the central nervous system to enhance inhibitory neurotransmission. - AZD0780 · AstraZeneca · GABA-A receptor positive allosteric modulator · Neurology
AZD0780 is a selective GABA-A receptor positive allosteric modulator that enhances inhibitory neurotransmission in the central nervous system. - Midazolam Nasal Spray · London Health Sciences Centre Research Institute OR Lawson Research Institute of St. Joseph's · Benzodiazepine · Neurology / Anesthesia
Midazolam is a benzodiazepine that enhances inhibitory GABA neurotransmission in the central nervous system to produce sedation and anxiolysis. - Clobazam Low Dose · Lundbeck LLC · Benzodiazepine anticonvulsant · Neurology
Clobazam is a benzodiazepine that enhances inhibitory GABAergic neurotransmission in the central nervous system to reduce seizure activity. - GSK1755165; placebo; zopiclone · GlaxoSmithKline · Non-benzodiazepine hypnotic (Z-drug) · Neurology / Sleep Medicine
GSK1755165 is a selective GABA-A receptor modulator that enhances inhibitory neurotransmission to promote sleep. - Sedation with midazolam · Consorci Sanitari de l'Anoia · Benzodiazepine · Anesthesia/Sedation
Midazolam is a benzodiazepine that enhances the inhibitory effects of GABA at the GABA-A receptor, depressing central nervous system activity to produce sedation. - Alprazolam orally disintegrating tablets · UCB Pharma · Benzodiazepine · Psychiatry/Neurology
Alprazolam is a benzodiazepine that enhances the inhibitory effects of GABA at the GABA-A receptor, reducing neuronal excitability and producing anxiolytic and sedative effects.
Phase 1 pipeline (1)
- Lusedra · Eisai Inc. · Other