Minaxolone (CCI-12923) is a neuroactive steroid which was developed as a general anesthetic but was withdrawn before registration due to toxicity seen with long-term administration in rats, and hence was never marketed.[1][2][3] It is a positive allosteric modulator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

Chemistry

See also

References

  1. ^ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1358–. ISBN 978-0-412-46630-4.
  2. ^ J. G. Bovill; Michael B. Howie (1999). Clinical Pharmacology for Anaesthetists. W.B. Saunders. ISBN 978-0-7020-2167-1.
  3. ^ Hugh C. Hemmings; Philip M. Hopkins (2006). Foundations of Anesthesia: Basic Sciences for Clinical Practice. Elsevier Health Sciences. pp. 305–. ISBN 978-0-323-03707-5.
  4. ^ a b Giovanni Biggio; Robert H. Purdy (2001). Neurosteroids and Brain Function. Academic Press. pp. 196–. ISBN 978-0-12-366846-2.
  5. ^ Weir CJ, Ling AT, Belelli D, Wildsmith JA, Peters JA, Lambert JJ (May 2004). "The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors". Br J Anaesth. 92 (5): 704–11. CiteSeerX 10.1.1.519.3591. doi:10.1093/bja/aeh125. PMID 15033889.