- 英文名称
- Arteether
- 分子式
- C17H28O5
- 分子量
- 312.4
- 中文别名
- 10-乙氧基十氢-3,6,9-三甲基-3,12-环氧-12H-吡喃并[4,3-j]-1,2-苯并二氧杂环庚烷; 青蒿素乙醚; 蒿醚; (3R,5AS,6R,8AS,9R,10S,12R,12AR)-10-乙氧基-3,6,9-三甲基十氢-3H-3,12-环氧[1,2]DIOXEPINO[4,3-I]异苯并呋喃; 阿格瑟; ARPRINOCID; SM-227; dihydroartemisinin ethyl ether; dihydroqinghaosu ethyl ether; (3R,12aR)-3,6α,9β-Trimethyl-10β-ethoxy-3β,12α-epoxy-3,4,5,5aα,6,7,8,8aα,9,10-decahydropyrano[4,3-j]-1,2-benzodioxepin; 3,12-Epoxy-12H-pyrano(4,3-J)-1,2-benzodioxepin, 10-ethoxydecahydro-3,6,9-trimethyl-, (3S-(3alpha,5alpha,6alpha,8aalpha,9beta,10beta,12beta,12aalpha))-; Artemotil; (4S,5R,8S,9R,10S,12R,13R)-10-Ethoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecane
- 用途
- - 简介
蒿乙醚为青蒿素的衍生物，作用同青蒿素，用于各种类型疟疾，也可用于不能口服其他抗疟药的患者。
- 作用
蒿乙醚可用于各种类型疟疾效果良好，疟原虫清除快，使用方便，也可用于不能口服其他抗疟药的患者。对疟原虫红内期有直接杀灭作用，对红前期及组织期无作用。
- 副作用
蒿乙醚的副作用包括：肌内注射部位疼痛，建议在两臀间更换注射部位。间歇性、非特异性的中枢神经紊乱，如头痛。胃肠系统功能紊乱，如腹部不适、呕吐。 大剂量长期使用青蒿素及其衍生物，可出现损害中枢神经系统和引起心电图变化两方面的毒理作用。对于中枢神经，损害部位特异，位于脑桥和髓质。
- 生物活性
Artemotil (β-Arteether) 具有抗疟疾活性，可用于研究耐 Plasmodium falciparum 的恶性疟原虫疟疾，IC50 值为 1.61 nM。Artemotiltil 对大鼠，狗和猴子具有 CNS 神经毒性和厌食毒性。
- 靶点
IC50: 1.61 nM (
Plasmodium falciparum
malaria)
- 体外研究
The antimalarial activity of Artemotil is test in vitro against chloroquine-resistant and chloroquine-sensitive
Plasmodium falciparum
parasites. The mean 50% inhibitory concentration (
IC
50
) for Artemotil is 1.61 nM (range 1.57-1.92 nM). Artemotil is approximately 2.5-fold more potent than artemisinin.
- 体内研究
Artemotil treatment (25 mg/kg; intravenous injection; daily; for 7 days; Sprague-Dawley male rats) shows anorectic toxicity and causes significant reductions in food consumption and body weight after day 2. AUC on day 7 is 5-fold higher than AUC on day 1. The elimination t
1/2
of Artemotil is also prolonged from 13.7 hours (day 1) to 31.2 hours (day 7).
Animal Model:
Sprague-Dawley male rats (220-280 g)
Dosage:
25 mg/kg; 1 mL/kg body weight
Administration:
Intravenous injection; daily; for 7 days
Result:
Anorectic toxicity was observed, and that caused significant reductions in food consumption and body weight after day 2.
