Minaxolone Explained

Minaxolone (CCI-12923) is a neuroactive steroid which was developed as a general anesthetic but was withdrawn before registration due to toxicity seen with long-term administration in rats, and hence was never marketed.[1] [2] [3] It is a positive allosteric modulator of the GABAA receptor,[4] as well as, less potently, a positive allosteric modulator of the glycine receptor.[5]

Chemistry

See also: List of neurosteroids.

See also

Notes and References

  1. Book: Ganellin CR, Triggle DJ . Dictionary of Pharmacological Agents. 21 November 1996. CRC Press. 978-0-412-46630-4. 1358–.
  2. Book: Bovill JB, Howie MC . Clinical Pharmacology for Anaesthetists. 1999. W.B. Saunders. 978-0-7020-2167-1 . 10.1016/B978-0-323-03707-5.50031-0 .
  3. Book: Perouansky MA, Hemmings Jr HC . Intravenous anesthetic agents . Hemmings HC, Hopkins PM . Foundations of Anesthesia: Basic Sciences for Clinical Practice. https://books.google.com/books?id=xaXu1wHmENoC&pg=PA305. 2006. Elsevier Health Sciences. 978-0-323-03707-5. 305–.
  4. Book: Lambert JJ, Harney SC, Belelli D, Peters JA . Neurosteroid modulation of recombinant and synaptic GABAA receptor. Biggio G, Purdy RH . Neurosteroids and Brain Function. https://books.google.com/books?id=13jQfYIkwhkC&pg=PA196. 2001. Academic Press. 978-0-12-366846-2. 196–.
  5. Weir CJ, Ling AT, Belelli D, Wildsmith JA, Peters JA, Lambert JJ . The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors . British Journal of Anaesthesia . 92 . 5 . 704–711 . May 2004 . 15033889 . 10.1093/bja/aeh125 . 10.1.1.519.3591 .