GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs.
Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil.
Other agents which may have GABAA receptor antagonism include the antibiotic ciprofloxacin, tranexamic acid,thujone,ginkgo biloba, and kudzu.
See also
External links
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| Ionotropic |
| GABAA |
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Positive modulators (abridged; see here for a full list): α-EMTBL
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Alcohols (e.g., drinking alcohol, 2M2B)
- Anabolic steroids
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Avermectins (e.g., ivermectin)
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Barbiturates (e.g., phenobarbital)
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Benzodiazepines (e.g., diazepam)
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Bromide compounds (e.g., potassium bromide)
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Carbamates (e.g., meprobamate)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
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Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
- Etazepine
- Etifoxine
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Fenamates (e.g., mefenamic acid)
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Flavonoids (e.g., apigenin, hispidulin)
- Fluoxetine
- Flupirtine
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Imidazoles (e.g., etomidate)
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Kava constituents (e.g., kavain)
- Lanthanum
- Loreclezole
- Monastrol
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Neuroactive steroids (e.g., allopregnanolone, cholesterol, THDOC)
- Niacin
- Niacinamide
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Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
- Norfluoxetine
- Petrichloral
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Phenols (e.g., propofol)
- Phenytoin
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Piperidinediones (e.g., glutethimide)
- Propanidid
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Pyrazolopyridines (e.g., etazolate)
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Quinazolinones (e.g., methaqualone)
- Retigabine (ezogabine)
- ROD-188
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Skullcap constituents (e.g., baicalin)
- Stiripentol
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Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
- Topiramate
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Valerian constituents (e.g., valerenic acid)
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Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, sevoflurane)
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Negative modulators: 1,3M1B
- 3M2B
- 11-Ketoprogesterone
- 17-Phenylandrostenol
- α5IA (LS-193,268)
- β-CCB
- β-CCE
- β-CCM
- β-CCP
- β-EMGBL
- Anabolic steroids
- Amiloride
- Anisatin
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β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
- Basmisanil
- Bemegride
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Bicyclic phosphates (TBPS, TBPO, IPTBO)
- BIDN
- Bilobalide
- Bupropion
- CHEB
- Chlorophenylsilatrane
- Cicutoxin
- Cloflubicyne
- Cyclothiazide
- DHEA
- DHEA-S
- Dieldrin
- (+)-DMBB
- DMCM
- DMPC
- EBOB
- Etbicyphat
- FG-7142 (ZK-31906)
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Fiproles (e.g., fipronil)
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Flavonoids (e.g., amentoflavone, oroxylin A)
- Flumazenil
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Fluoroquinolones (e.g., ciprofloxacin)
- Flurothyl
- Furosemide
- Golexanolone
- Iomazenil (123I)
- IPTBO
- Isopregnanolone (sepranolone)
- L-655,708
- Laudanosine
- Leptazol
- Lindane
- MaxiPost
- Morphine
- Morphine-3-glucuronide
- MRK-016
- Naloxone
- Naltrexone
- Nicardipine
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Nonsteroidal antiandrogens (e.g., apalutamide, bicalutamide, enzalutamide, flutamide, nilutamide)
- Oenanthotoxin
- Pentylenetetrazol (pentetrazol)
- Phenylsilatrane
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Picrotoxin (i.e., picrotin, picrotoxinin and dihydropicrotoxinin)
- Pregnenolone sulfate
- Propybicyphat
- PWZ-029
- Radequinil
- Ro 15-4513
- Ro 19-4603
- RO4882224
- RO4938581
- Sarmazenil
- SCS
- Suritozole
- TB-21007
- TBOB
- TBPS
- TCS-1105
- Terbequinil
- TETS
- Thujone
- U-93631
- Zinc
- ZK-93426
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| GABAA-ρ |
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| Metabotropic |
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