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- alphaxalone
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/04/25 06:07:00」(JST)
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Alfaxalone
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Systematic (IUPAC) name |
3-hydroxypregnane-11,20-dione |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
Pregnancy cat. |
? |
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 N |
ATC code |
N01AX05 |
PubChem |
CID 104845 |
ChemSpider |
94637 Y |
UNII |
BD07M97B2A Y |
KEGG |
D07282 Y |
ChEMBL |
CHEMBL190279 Y |
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
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InChI
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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 Y
Key:DUHUCHOQIDJXAT-OLVMNOGESA-N Y
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N (what is this?) (verify)
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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 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
References
- ^ "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
Hypnotics/sedatives (N05C)
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GABAA
agonists/PAMs |
Alcohols: 2M2B • Chloralodol • Ethanol (Alcohol) • Ethchlorvynol • Methylpentynol • Trichloroethanol
Barbiturates: Allobarbital • Amobarbital • Aprobarbital • Barbital • Butabarbital • Butobarbital • Cyclobarbital • Ethallobarbital • Heptabarb • Hexobarbital • Mephobarbital • Methohexital • Pentobarbital • Phenallymal • Phenobarbital • Propylbarbital • Proxibarbal • Reposal • Secobarbital • Talbutal • Thiamylal • Thiopental • Vinbarbital • Vinylbital
Benzodiazepines: Brotizolam • Clonazepam • Cinolazepam • Climazolam • Doxefazepam • Estazolam • Flunitrazepam • Flurazepam • Flutoprazepam • Haloxazolam • Loprazolam • Lorazepam •Lormetazepam • Midazolam • Nimetazepam • Nitrazepam • Quazepam • Temazepam • Triazolam
Carbamates: Carisoprodol • Ethinamate • Hexapropymate • Meprobamate • Methocarbamol • Procymate • Tybamate
Neuroactive Steroids: Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Eltanolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • Org 21465 • Tetrahydrodeoxycorticosterone
Nonbenzodiazepines: CL-218,872 • Eszopiclone • Indiplon • JM-1232 • Lirequinil • Necopidem • Pazinaclone • ROD-188 • Saripidem • Suproclone • Suriclone • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiclone
Phenols: Fospropofol • Propofol
Piperidinediones: Glutethimide • Methyprylon • Pyrithyldione • Piperidione
Quinazolinones: Afloqualone • Cloroqualone • Diproqualone • Etaqualone • Mebroqualone • Mecloqualone • Methaqualone • Methylmethaqualone • Nitromethaqualone • SL-164
Volatiles/gases: • Acetophenone • Acetylglycinamide chloral hydrate • Centalun • Chloral hydrate • Paraldehyde
Others: Bromide (Lithium bromide, Potassium bromide, Sodium bromide) • Chloralose • Clomethiazole • Dichloralphenazone • Etomidate • Gaboxadol • Loreclezole • Metomidate • Org 25435 • Petrichloral • Sulfonmethane • Triclofos • Valerenic acid (Valerian)
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GABAB
agonists |
1,4-Butanediol • Aceburic acid • GABOB • GHB (Sodium oxybate) • GBL • GVL
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H1 inverse
agonists |
Antihistamines: Captodiame • Cyproheptadine • Diphenhydramine • Doxylamine • Hydroxyzine • Methapyrilene • Pheniramine • Promethazine • Propiomazine
Antidepressants: Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
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α1-Adrenergic
antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Niaprazine
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α2-Adrenergic
agonists |
4-NEMD • Clonidine • Detomidine • Dexmedetomidine • Lofexidine • Medetomidine • Romifidine • Tizanidine • Xylazine
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5-HT2A
antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Eplivanserin • Niaprazine • Pruvanserin • Volinanserin
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Melatonin
agonists |
Agomelatine • LY-156,735 • Melatonin • Ramelteon • Tasimelteon
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Orexin
antagonists |
Almorexant • SB-334,867 • SB-408,124 • SB-649,868 • Suvorexant • TCS-OX2-29
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Others |
Acecarbromal • Apronal • Bromisoval • Cannabidiol (Cannabis) • Carbromal • Embutramide • Evoxine • Fenadiazole • Gabapentin • Kavalactones (Kava) • Mephenoxalone • Opioids (Oxycodone, Morphine (Opium), etc.) • Passion flower • Scopolamine (Mandrake) • UMB68 • Valnoctamide
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Anesthetic: General anesthetics (N01A)
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Inhalation |
Ethers
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- Diethyl ether
- Methoxypropane
- Vinyl ether
- halogenated ethers
- Desflurane
- Enflurane
- Isoflurane
- Methoxyflurane
- Sevoflurane
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Haloalkanes
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- Chloroform
- Halothane#
- Trichloroethylene
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Others
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- Cyclopropane
- Ethylene
- Nitrous oxide#
- Xenon
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Injection |
Barbiturates
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- Hexobarbital
- Methohexital
- Narcobarbital
- Thiopental#
- Thiotetrabarbital
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Opioids
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- Alfentanil
- Anileridine
- Fentanyl
- Phenoperidine
- Remifentanil
- Sufentanil
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Neuroactive steroids
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Others
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- Droperidol
- Etomidate
- Fospropofol
- gamma-Hydroxybutyric acid
- Ketamine# /Esketamine
- Midazolam
- Propanidid
- Propofol
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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anat (n/s/m/p/4/e/b/d/c/a/f/l/g)/phys/devp
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noco (m/d/e/h/v/s)/cong/tumr, sysi/epon, injr
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proc, drug (N1A/2AB/C/3/4/7A/B/C/D)
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GABAergics
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Receptor
ligands |
GABAA
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- Agonists: Main site: Bamaluzole
- Gaboxadol
- Ibotenic acid
- Isoguvacine
- Isonipecotic acid
- Muscimol (Amanita Muscaria)
- Progabide
- SL 75102
- Thiomuscimol
- Tolgabide; Positive allosteric modulators: Alcohols (2M2B, Ethanol, Ethchlorvynol, Methylpentynol
- Barbiturates
- Benzodiazepines
- Carbamates
- Chlormezanone
- Clomethiazole
- Etomidate
- Kavalactones (Kava)
- Loreclezole
- Metomidate
- Neuroactive steroids
- Nonbenzodiazepines (β-Carbolines, Cyclopyrrolones, Imidazopyridines, Pyrazolopyrimidines, etc.)
- Phenols
- Piperidinediones
- Propanidid
- Pyrazolopyridines
- Quinazolinones
- ROD-188
- Skullcap
- Stiripentol
- Valerenic acid (Valerian)
Note: See the GABAA receptor PAMs navbox for a full list of GABAA positive allosteric modulators.
- Antagonists: Main site: Bicuculline
- Gabazine
- Pitrazepin
- Quisqualamine; Negative allosteric modulators: 17-Phenylandrostenol (17-PA)
- α5IA
- Bilobalide
- Cicutoxin
- Cyclothiazide
- DMCM
- Flumazenil
- Flurothyl
- Furosemide
- Iomazenil (123I)
- L-655,708
- Oenanthotoxin
- Penicillin
- Pentylenetetrazol
- Picrotoxin
- PWZ-029
- Radequinil
- Ro15-4513
- Sarmazenil
- Suritozole
- Terbequinil
- Thujone
- Thiocolchicoside
- ZK-93426
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GABAB
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- Agonists: Main site: 1,4-Butanediol
- Baclofen
- GBL
- GHB
- GHV
- GVL
- Lesogaberan
- Phenibut
- Progabide
- SKF-97,541
- Tolgabide; Positive allosteric modulators: BHF-177
- BHFF
- BSPP
- CGP-7930
- GS-39783
Antagonists: Main site: CGP-35348
- Phaclofen
- Saclofen
- SCH-50911
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GABAC
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- Agonists: Main site: CACA
- CAMP
- GABOB
- N4-Chloroacetylcytosine arabinoside
- Progabide
- Tolgabide
Antagonists: Main site: Bilobalide
- TPMPA
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Reuptake
inhibitors |
Plasmalemmal
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GAT inhibitors
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- CI-966
- Deramciclane
- EF-1502
- Gabaculine
- Guvacine
- Nipecotic acid
- NNC 05-2090
- SKF-89976A
- SNAP-5114
- Tiagabine
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Enzyme
inhibitors |
Anabolism
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Catabolism
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GABA-T inhibitors
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- 3-Hydrazinopropionic acid
- Aminooxyacetic acid
- Gabaculine
- Isoniazid
- Phenelzine
- Phenylethylidenehydrazine
- Sodium valproate
- Valnoctamide
- Valproate pivoxil
- Valproate semisodium (Divalproex sodium)
- Valproic acid
- Valpromide
- Vigabatrin
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Others |
Precursors
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Cofactors
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- Vitamin B6 (pyridoxine
- pyridoxamine
- pyridoxal phosphate)
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Others
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- Gabapentin
- Hopantenic acid
- Picamilon
- Pregabalin
- L-Theanine
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English Journal
- An alternative method of endotracheal intubation of common marmosets (Callithrix jacchus).
- Thomas AA, Leach MC, Flecknell PA.SourceInstitute of Neuroscience and Comparative Biology Centre, Medical School, Newcastle University, Framlington Place, Newcastle upon Tyne NE2 4HH, UK.
- Laboratory animals.Lab Anim.2011 Nov 2. [Epub ahead of print]
- Endotracheal intubation was carried out in 11 common marmosets (Callithrix jacchus). A commercially available tilting stand and a Miller laryngoscope blade were used to visualize the larynx. Anaesthesia was induced with alphaxalone (10.6 ± 1.6 mg/kg intramuscularly, followed by 3.2 ± 1.2 mg/kg int
- PMID 22048957
- Immersion and branchial/transcutaneous irrigation anaesthesia with alfaxalone in a Mexican axolotl.
- McMillan MW, Leece EA.SourceDepartment of Veterinary Medicine, University of Cambridge, Cambridge, UK.
- Veterinary anaesthesia and analgesia.Vet Anaesth Analg.2011 Nov;38(6):619-23. doi: 10.1111/j.1467-2995.2011.00660.x.
- INTRODUCTION: Immersion anaesthetic techniques are commonly used in amphibian species. Alfaxalone has been reported as an immersion anaesthetic in fish but not amphibians. CASEHISTORY AND EXAMINATION: A Mexican 56 g axolotl was presented with a 3-day history of anorexia. Anaesthesia was required f
- PMID 21988819
Related Links
- VASG Anesthesia Guidebook Admissions Preanesthetic Routine Preanesthetic Protocols Anesthetic Induction Anesthetic Induction Protocols Anesthetic Maintenance Anesthetic Maintenance Protocols Recovery Alfaxalone - NEW!!
- vii Comparison of the anesthetic efficacy and cardiopulmonary effects of continuous rate infusions of alfaxalone-2-hydroxypropyl-beta-cyclodextrin and propofol in dogs. Ambros B, Duke-Novakovski T, Pasloske KS. Am J Vet Res ...
Related Pictures
★リンクテーブル★
[★]
- 英
- alphaxalone、alfaxalone
-alphaxalone
[★]
アルファキサロン
- 関
- alfaxalone
[★]
アルファキサロン・アルファドロン混合物