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Tribendimidine 一种广谱的、具有口服活性的驱虫剂,对 A. lumbricoides 和 N. americanus 具有特别高的活性。Tribendimidine 也是 L 型烟碱乙酰胆碱受体 (nAChR) 激动剂。
Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist[1][2][3].
Tribendimidine (100 μg/mL; 24 h) shows intoxication of C. elegans[3].
Tribendimidine (0-100 μg/mL; 6 days) shows toxicity with an LC50 value (concentration at which half the animals are dead) of 54.4 μg/mL[3].
Tribendimidine (0-200 μg/mL; 64 h)-induced sterility is resisted by trb mutant hermaphrodites, and Levamisole-resistant mutants are resistant to Tribendimidine. [3].
Tribendimidine (75 and 150 mg/kg; p.o.; once) shows inhibition activity against C. sinensis in rats, and shows inhibition against O. viverrini at 400 mg/kg in hamsters[2].
Animal Model: | C. sinensis infected Female Wistar rats[2] |
Dosage: | 75 mg/kg and 150 mg/kg |
Administration: | Oral administration, once |
Result: | A 99.1% worm burden reduction was achieved at 150 mg/kg, and the worm burden reduction was still significant (68.9%) at 75 mg/kg. |
[1]. Xiao SH, et al. Tribendimidine: a promising, safe and broad-spectrum anthelmintic agent from China. Acta Trop. 2005 Apr;94(1):1-14.
[2]. Keiser J, et al. Evaluation of the in vivo activity of tribendimidine against Schistosoma mansoni, Fasciola hepatica, Clonorchis sinensis, and Opisthorchis viverrini. Antimicrob Agents Chemother. 2007 Mar;51(3):1096-8.
[3]. Hu Y, et al. The new anthelmintic tribendimidine is an L-type (levamisole and pyrantel) nicotinic acetylcholine receptor agonist. PLoS Negl Trop Dis. 2009 Aug 11;3(8):e499.
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