GABA receptor antagonist

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 GABA_A receptor antagonist flumazenil.

Other agents which may have GABA_A receptor antagonism include the antibiotic ciprofloxacin,^[1] tranexamic acid,^[2] thujone,^[3] ginkgo biloba,^[4] and kudzu.^[5]

See also

GABA_A receptor negative allosteric modulators

External links

GABA+antagonists at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

References

^ Green, M. A.; Halliwell, R. F. (October 1997). "Selective antagonism of the GABA A receptor by ciprofloxacin and biphenylacetic acid". British Journal of Pharmacology. 122 (3): 584–590. doi:10.1038/sj.bjp.0701411. ISSN 0007-1188. PMC 1564969. PMID 9351519.
^ Roman Furtmüller; Michael G Schlag; Michael Berger; Rudolf Hopf; Sigismund Huck; Werner Sieghart; Heinz Redl (April 2002). "Tranexamic Acid, a Widely Used Antifibrinolytic Agent, Causes Convulsions by a γ-Aminobutyric Acid_A Receptor Antagonistic Effect". Journal of Pharmacology and Experimental Therapeutics. 301 (1): 168–173. doi:10.1124/jpet.301.1.168. PMID 11907171. Retrieved 1 November 2021.
^ Karin M. Höld; Nilantha S. Sirisoma; Tomoko Ikeda; Toshio Narahashi; John E. Casida (April 2000). "α-Thujone (the active component of absinthe): γ-Aminobutyric acid type A receptor modulation and metabolic detoxification". PNAS. 97 (8): 3826–3831. Bibcode:2000PNAS...97.3826H. doi:10.1073/pnas.070042397. PMC 18101. PMID 10725394.
^ Lidija Ivic; Tristan T.J. Sands; Nathan Fishkin; Koji Nakanishi; Arnold R. Kriegstein; Kristian Strømgaard (December 2003). "Terpene Trilactones from Ginkgo biloba Are Antagonists of Cortical Glycine and GABA_A Receptors". Journal of Biological Chemistry. 278 (49): 49279–49285. doi:10.1074/jbc.M304034200. PMID 14504293. Retrieved 1 November 2021.
^ Robert M. Swift; Elizabeth R. Aston (March 2015). "Pharmacotherapy for Alcohol Use Disorder: Current and Emerging Therapies". Harvard Review of Psychiatry. 23 (2): 122–133. doi:10.1097/HRP.0000000000000079. PMC 4790835. PMID 25747925.

GABA receptor modulators

Positive modulators (abridged; see here for a full list): α-EMTBL
Alcohols (e.g., drinking alcohol, 2M2B)
Anabolic steroids
Avermectins (e.g., ivermectin)
Barbiturates (e.g., phenobarbital)
Benzodiazepines (e.g., diazepam)
Bromide compounds (e.g., potassium bromide)
Carbamates (e.g., meprobamate)
Carbamazepine
Chloralose
Chlormezanone
Clomethiazole
Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
Etazepine
Etifoxine
Fenamates (e.g., mefenamic acid)
Flavonoids (e.g., apigenin, hispidulin)
Fluoxetine
Flupirtine
Imidazoles (e.g., etomidate)
Kava constituents (e.g., kavain)
Lanthanum
Loreclezole
Monastrol
Neuroactive steroids (e.g., allopregnanolone, cholesterol, THDOC)
Niacin
Niacinamide
Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
Norfluoxetine
Petrichloral
Phenols (e.g., propofol)
Phenytoin
Piperidinediones (e.g., glutethimide)
Propanidid
Pyrazolopyridines (e.g., etazolate)
Quinazolinones (e.g., methaqualone)
Retigabine (ezogabine)
ROD-188
Skullcap constituents (e.g., baicalin)
Stiripentol
Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
Topiramate
Valerian constituents (e.g., valerenic acid)
Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, sevoflurane)

Negative modulators: 5α-Dihydroprogesterone
Bilobalide
Loreclezole
Picrotoxin (picrotin, picrotoxinin)
Pregnanolone
ROD-188
THDOC
Zinc

Negative modulators: Compound 14

See also: Receptor/signaling modulators; GABA_A receptor positive modulators; GABA metabolism/transport modulators

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