Minaxolone

Minaxolone

Minaxolone
Systematic (IUPAC) name
(2β,3α,5α,11α)-11-(dimethylamino)-2-ethoxy-3-hydroxypregnan-20-one
Clinical data
Legal status
?
Identifiers
CAS number  YesY
ATC code None
PubChem
ChemSpider  N
UNII  YesY
KEGG  YesY
ChEMBL  N
Synonyms 1-[(1S,2S,4S,5S,7S,10S,11S,14S,15S,17R)-17-(dimethylamino)-4-ethoxy-5-hydroxy-2,15-dimethyltetracyclo[8.7.0.02,7.011,15]heptadecan-14-yl]ethan-1-one
Chemical data
Formula C25H43NO3 
Mol. mass 405.614 g/mol
 N   

Minaxolone (CCI-12923) is a neuroactive steroid which was developed as a general anesthetic but was withdrawn before registration due to toxicity seen with long-term administration in rats, and hence was never marketed.[1][2][3] It is a positive allosteric modulator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

See also

References

  1. ^ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 1358–.  
  2. ^ J. G. Bovill; Michael B. Howie (1999). Clinical Pharmacology for Anaesthetists. W.B. Saunders.  
  3. ^ Hugh C. Hemmings; Philip M. Hopkins (2006). Foundations of Anesthesia: Basic Sciences for Clinical Practice. Elsevier Health Sciences. pp. 305–.  
  4. ^ a b Giovanni Biggio; Robert H. Purdy (2001). Neurosteroids and Brain Function. Academic Press. pp. 196–.  
  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.