GABA receptor antagonist explained

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,[1] tranexamic acid,[2] thujone,[3] ginkgo biloba,[4] and kudzu.[5]

See also

Notes and References

  1. Green . M. A. . Halliwell . R. F. . October 1997 . Selective antagonism of the GABA A receptor by ciprofloxacin and biphenylacetic acid . British Journal of Pharmacology . en . 122 . 3 . 584–590 . 10.1038/sj.bjp.0701411 . 0007-1188 . 1564969 . 9351519.
  2. Tranexamic Acid, a Widely Used Antifibrinolytic Agent, Causes Convulsions by a γ-Aminobutyric AcidA Receptor Antagonistic Effect. Roman Furtmüller. Michael G Schlag. Michael Berger. Rudolf Hopf. Sigismund Huck. Werner Sieghart. Heinz Redl. Journal of Pharmacology and Experimental Therapeutics. 10.1124/jpet.301.1.168. 301. 1. 168–173. April 2002. 11907171. 1 November 2021.
  3. PNAS. α-Thujone (the active component of absinthe): γ-Aminobutyric acid type A receptor modulation and metabolic detoxification. 10.1073/pnas.070042397. free. Karin M. Höld. Nilantha S. Sirisoma. Tomoko Ikeda. Toshio Narahashi. John E. Casida. April 2000. 97. 8. 3826–3831. 10725394. 18101. 2000PNAS...97.3826H.
  4. Terpene Trilactones from Ginkgo biloba Are Antagonists of Cortical Glycine and GABAA Receptors. Lidija Ivic. Tristan T.J. Sands. Nathan Fishkin. Koji Nakanishi. Arnold R. Kriegstein. Kristian Strømgaard. 10.1074/jbc.M304034200. free. Journal of Biological Chemistry. 278. 49. 49279–49285. December 2003. 14504293 . 1 November 2021.
  5. 4790835. 25747925. 10.1097/HRP.0000000000000079. free. Pharmacotherapy for Alcohol Use Disorder: Current and Emerging Therapies. Robert M. Swift. Elizabeth R. Aston. Harvard Review of Psychiatry. March 2015. 23. 2. 122–133.

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