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ChemicalBook Optimization Suppliers |
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| 化学名: | アルファキサロン | | 英語化学名: | Alfaxalone | | 别名: | 3ALPHA-HYDROXY-5ALPHA-PREGNANE-11,20-DIONE;3-HYDROXY-5ALPHA-PREGNANE-11,20-DIONE;5ALPHA-PREGNAN-3ALPHA-OL-11,20-DIONE;ALFAXALONE;ALPHAXALONE;(3-alpha,5-alpha)-3-hydroxypregnane-11,20-dione;20-dione,3-alpha-hydroxy-5-alpha-pregnane-1;20-dione,3-hydroxy-,(3-alpha,5-alpha)-pregnane-1 | | CAS番号: | 23930-19-0 | | 分子式: | C21H32O3 | | 分子量: | 332.48 | | EINECS: | | | カテゴリ情報: | | | Mol File: | 23930-19-0.mol |  |
| 融点 | 172-174° | | 比旋光度 | D26 +113.4° (c = 1.2 in chloroform). | | 沸点 | 409.59°C (rough estimate) | | 比重(密度) | 1.0834 (rough estimate) | | 屈折率 | 1.5192 (estimate) | | 貯蔵温度 | Store at RT | | 溶解性 | chloroform: ≥5 mg/mL, clear, colorless | | 外見 | powder | | 酸解離定数(Pka) | 15.05±0.70(Predicted) | | 色 | white | | InChI | InChI=1/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+/s3 | | InChIKey | DUHUCHOQIDJXAT-YYJIQYHHNA-N | | SMILES | [C@]12([H])C(=O)C[C@]3(C)[C@H](CC[C@@]3([H])[C@]1([H])CC[C@@]1([H])C[C@H](O)CC[C@]21C)C(=O)C |&1:0,5,7,10,12,16,19,23,r| |
| 主な危険性 | Xn | | Rフレーズ | 22 | | Sフレーズ | 22-36 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | RTECS 番号 | TU4157800 | | 毒性 | LD50 i.v. in mice: 43 mg/kg (Al-Khawashki) |
| | アルファキサロン Usage And Synthesis |
| 効能 | 麻酔薬 | | 説明 | Alfaxalone (Alfaxan, Vetoquinol) is a neurologically active steroid compound that induces general anaesthesia. Alfaxalone exerts its action by binding to GABA receptors on the neuronal cell surface, affecting cell membrane chloride ion transport. It has negligible analgesic properties at therapeutic doses. Alfaxalone may be administered either intravenously or intramuscularly, and due to the possibility of apnoea after intravenous induction this route should be reserved for cases where intubation can be achieved[2]. | | Originator | Althesin ,Glaxo ,UK ,1972 | | 使用 | Anesthetic;nociception blocker | | 定義 | ChEBI: Alphaxolone is a corticosteroid hormone. | | Manufacturing Process | A solution of 3α-hydroxy-5α-pregn-16-ene-11,20-dione (200 mg) in freshly
distilled tetrahydrofuran (8 ml) with 5% palladium on carbon (100 ml) was
hydrogenated until hydrogen uptake ceased. The mixture was filtered through
a pad of kieselguhr and the tetrahydrofuran removed in vacuum to give 196
mg, MP 171°C to 172°C. | | Therapeutic Function | Anesthetic component | | 生物活性 | A neurosteroid anesthetic that directly activates and potentiates GABA A receptor-activated membrane current (I GABA ). Efficacy but not potency is determined by the alpha subunit of the receptor (EC 50 values are 1.4, 1.8, 2.1, 2.4 and 2.5 μ M for α 1 β 1 γ 3, α 1 β 1 γ 1, β 1 γ 1, α 2 β 1 γ 2L and α 1 β 1 γ 2L isoforms respectively). | | 作用機序 | Alfaxalone's mechanism of action is chloride ion modulation associated with interaction with the neuronal membrane GABA A receptor[1]. | | 副作用 | Alfaxalone is safe and effective at 12–15 mg/kg IM for routine noninvasive procedures and lasts approximately 40–45 min. The most common side effects are dose-dependent but transient hypotension (15 min), hypoventilation, and apnea. Higher doses of alfaxalone (12 mg/kg) may cause mild hypoxemia, which can be corrected by administration of supplemental oxygen via face mask. Muscle twitching occurs toward the end of immobilization and can be used as a sign of impending emergence[1]. | | 合成 | It is prepared by
reduction of 3,11,20-trioxo-5-α-pregnane with
trimethyl phosphite in the presence of an iridium
catalyst. Only this reducing agent forms the
axial alcohol (3α) .
 | | 参考文献 |
[1] Marini, R. and J. Haupt. “Anesthesia and Select Surgical Procedures.” The Common Marmoset in Captivity and Biomedical Research 61 1 (2019).
[2] Molly Varga BVetMed DZooMed MRCVS. “Anaesthesia and Analgesia.” Textbook of Rabbit Medicine (Second Edition) (2014): 178-202.
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