75887-54-6
75887-54-6 結(jié)構(gòu)式
基本信息
10-乙氧基十氫-3,6,9-三甲基-3,12-環(huán)氧-12H-吡喃并[4,3-j]-1,2-苯并二氧雜環(huán)庚烷
SM-227
Areether
Artemotil
Arteether
ARPRINOCID
aArteether
NSC 665971
Unii-xgl7gfb9yi
Alpha Beta Arteether
物理化學(xué)性質(zhì)
常見問題列表
蒿乙醚為青蒿素的衍生物，作用同青蒿素，用于各種類型瘧疾，也可用于不能口服其他抗瘧藥的患者。
蒿乙醚可用于各種類型瘧疾效果良好，瘧原蟲清除快，使用方便，也可用于不能口服其他抗瘧藥的患者。對(duì)瘧原蟲紅內(nèi)期有直接殺滅作用，對(duì)紅前期及組織期無作用。
蒿乙醚的副作用包括：肌內(nèi)注射部位疼痛，建議在兩臀間更換注射部位。間歇性、非特異性的中樞神經(jīng)紊亂，如頭痛。胃腸系統(tǒng)功能紊亂，如腹部不適、嘔吐。 大劑量長(zhǎng)期使用青蒿素及其衍生物，可出現(xiàn)損害中樞神經(jīng)系統(tǒng)和引起心電圖變化兩方面的毒理作用。對(duì)于中樞神經(jīng)，損害部位特異，位于腦橋和髓質(zhì)。
IC50: 1.61 nM ( Plasmodium falciparum malaria)
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.
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. |