Alfaxalone

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Alfaxalone
Alphaxolone.svg
Systematic (IUPAC) name
3α-hydroxy-5α-pregnane-11,20-dione
Clinical data
AHFS/Drugs.com International Drug Names
Legal status
Pharmacokinetic data
Bioavailability The alfaxalone molecule is solubilised using SBECD. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
Identifiers
CAS number 23930-19-0 N
ATC code N01AX05
PubChem CID 104845
ChemSpider 94637 YesY
UNII BD07M97B2A YesY
KEGG D07282 YesY
ChEMBL CHEMBL190279 YesY
Chemical data
Formula C21H32O3 
Mol. mass 332.477 g/mol
 N (what is this?)  (verify)

Alfaxalone (INN, also known as alphaxalone or alphaxolone) is a neurosteroid general anaesthetic.

It is one of the constituents of althesin.

It is used in veterinary practice under the tradename Alfaxan. [1]

It is licensed for use in both dogs and cats.[citation needed]

Unlike some of its predecessors alfaxalone is not associated with histamine release and anaphylaxis.[citation needed]

A study 1987 found the primary mechanism for the anaesthetic action of alfaxalone to be modulation of neuronal cell membrane chloride ion transport, induced by binding of alfaxalone to GABAA cell surface receptors. [2]

A 1994 study found that alfaxalone binds to a different region of this receptor than the benzodiazepines. [3]

Alfaxalone is metabolised rapidly in the liver. Alfaxalone has a very short plasma elimination half-life in dogs and cats.[citation needed]

See also[edit]

References[edit]

  1. ^ "Alfaxalone". Drugs.com. 
  2. ^ Harrison, N. L.; Vicini, S.; Barker, J. L. (1987). "A steroid anesthetic prolongs inhibitory postsynaptic currents in cultured rat hippocampal neurons" (pdf). The Journal of neuroscience 7 (2): 604–609. PMID 3819824.  edit
  3. ^ Mihic, S. J.; Whiting, P. J.; Klein, R. L.; Wafford, K. A.; Harris, R. A. (1994). "A single amino acid of the human gamma-aminobutyric acid type A receptor gamma 2 subunit determines benzodiazepine efficacy" (pdf). The Journal of Biological Chemistry 269 (52): 32768–32773. PMID 7806498.  edit