GABA receptor antagonist

Last updated

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.

Contents

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

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. 122 (3): 584–590. doi:10.1038/sj.bjp.0701411. ISSN   0007-1188. PMC   1564969 . PMID   9351519.
  2. ↑ 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 AcidA 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.
  3. ↑ 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.
  4. ↑ 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 GABAA Receptors". Journal of Biological Chemistry . 278 (49): 49279–49285. doi: 10.1074/jbc.M304034200 . PMID   14504293.
  5. ↑ 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.


This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.