36531-26-7
36531-26-7 结构式
基本信息
中文别名
间酚嘧啶奥克太尔
奥克生太
英文别名
OXANTELTelopar
CP-14445-16
OXANTEL USP/EP/BP
3-[(E)-2-(1-methyl-5,6-dihydro-4H-pyrimidin-2-yl)ethenyl]phenol
(E)-3-(2-(1,4,5,6-Tetrahydro-1-methyl-2-pyrimidinyl)vinyl)phenol
3-[(E)-2-(1,4,5,6-Tetrahydro-1-methylpyrimidin-2-yl)vinyl]phenol
Phenol, 3-[(1E)-2-(1,4,5,6-tetrahydro-1-methyl-2-pyrimidinyl)ethenyl]-
所属类别
原料药：驱肠虫药常见问题列表
生物活性
Oxantel (CP-14445) 是 Pyrantel (HY-12641) 的衍生物，是 N-亚型的 AChR 激动剂。Oxantel 是一种驱虫剂，具有优良驱虫活性。靶点
nAChR
体外研究
Oxantel ( 0.015-600 µg/mL; 24-72 hours) reduces the viability of
T. muris
.
Cell Viability Assay
| Cell Line: | T. muris |
| Concentration: | 0.015 µg/mL, 0.3 µg/mL, 0.6 µg/mL, 4.66 µg/mL, 9.375 µg/mL, 150 µg/mL, 600 µg/mL |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Resulted in strongly reduced viabilities; resulted in strongly reduced viabilities within 24 hours but did not kill the worms. |
体内研究
Oxantel (1-10 mg/kg; i.p.) displays a high activity against
T. muris
in vivo, with an EC
50
of 4.71 mg/kg.
Oxantel (10 mg/kg; i.p.) exhibits a worm burden reduction (WBR) of 92.5% and worm expulsion rate (WER) of 88.4% for
T. muris
.
| Animal Model: | 4 week-old female C57BL/10 mice and 3 week-old male |
| Dosage: | 1 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Inhibited T. muris in vivo. |