関: alfaxalone

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/19 15:28:02」(JST)

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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 GABA_A 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]}

References[edit]

^ "Alfaxalone". Drugs.com.
^ 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
^ 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

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English Journal

The effect of alphaxalone-alphadolone, propofol, and pentobarbitone anaesthesia on the β-endorphin and ACTH response to haemorrhage in the pig.

Ruane-O'Hora T, Hall WJ, Markos F.SourceDepartment of Physiology, University College Cork, Cork, Ireland.
Canadian journal of physiology and pharmacology.Can J Physiol Pharmacol.2011 Jul;89(7):521-6.
In the literature there appears to be variability in reported levels of certain hormones during haemorrhage, specifically adrenocorticotrophic hormone (ACTH) and β-endorphin. It is possible that this variability may be due to the choice of anaesthetic. Therefore, the effect of 3 common research-onl
PMID 21812530

Neurosteroid analogues. 16. A new explanation for the lack of anesthetic effects of δ(16)-alphaxalone and identification of a δ(17(20)) analogue with potent anesthetic activity.

Stastna E, Krishnan K, Manion BD, Taylor A, Rath NP, Chen ZW, Evers AS, Zorumski CF, Mennerick S, Covey DF.SourceDepartment of Developmental Biology, Washington University in St. Louis School of Medicine, St. Louis, MO 63110, USA.
Journal of medicinal chemistry.J Med Chem.2011 Jun 9;54(11):3926-34. Epub 2011 May 6.
This study addresses the hypothesis that the lack of anesthetic activity for (3α,5α)-3-hydroxypregn-16-ene-11,20-dione (Δ(16)-alphaxalone) is explained by the steroid Δ(16) double bond constraining the steroid 20-carbonyl group to a position that prevents it from favorably interacting with γ-am
PMID 21504158

Japanese Journal

Mechanism-based pharmacokinetic-pharmacodynamic modeling of concentration dependent hysteresis and biphasic electroencephalogram effects of alphaxalone in rats

VISSER SAG
J Pharmacol Exp Ther 302, 1158-1167, 2002
NAID 30003045037

High-performance liquid chromatography of the neuroactive steroids alphaxalone and pregnanolone in plasma using dansyl hydrazine as fluorescent label : application to a pharmacokinetic-pharmacodynamic study in rats

VISSER Sandra A. G.,SMULDERS Chantal J. G. M.,GLADDINES Werner W. F. T.,IRTH Hubertus,VAN DER GRAAF Piet H.,DANHOF Meindert
Journal of chromatography. B, Biomedical applications 745(2), 357-363, 2000-08-18
NAID 10012267554

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リンク元	「アルファキサロン」「alfaxalone」

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Alfaxalone
Systematic (IUPAC) name
	3-hydroxypregnane-11,20-dione
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	?
Pharmacokinetic data
Bioavailability	The alfaxalone molecule is solubilised in the Alfaxan formulation using 2α- hydroxypropyl β cyclodextrin. Cyclodextrins are complex polysaccharides derived from starch that supply a hydrophobic centre for lipophilic drugs like alfaxalone.
Identifiers
CAS number	23930-19-0
ATC code	N01AX05
PubChem	CID 104845
ChemSpider	94637
UNII	BD07M97B2A
KEGG	D07282
ChEMBL	CHEMBL190279
Chemical data
Formula	C21H32O3
Mol. mass	332.477 g/mol
	SMILES O=C2[C@H]3[C@H]([C@@H]1CC[C@H](C(=O)C)[C@@]1(C)C2)CC[C@H]4C[C@H](O)CC[C@]34C;
	InChI InChI=1S/C21H32O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h13-17,19,23H,4-11H2,1-3H3/t13-,14+,15-,16+,17-,19+,20-,21+/m0/s1 ; Key:DUHUCHOQIDJXAT-OLVMNOGESA-N ;
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