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tribendimidine

Names

[ CAS No. ]:
115103-15-6

[ Name ]:
tribendimidine

[Synonym ]:
Tribendimidine
Tribendimidin

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR
Signaling Pathways >> Neuronal Signaling >> nAChR

[In Vitro]

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].

[In Vivo]

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.

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.04g/cm3

[ Boiling Point ]:
618.2ºC at 760mmHg

[ Molecular Formula ]:
C28H32N6

[ Molecular Weight ]:
452.59400

[ Flash Point ]:
327.7ºC

[ Exact Mass ]:
452.26900

[ PSA ]:
55.92000

[ LogP ]:
6.41080

[ Vapour Pressure ]:
3.26E-15mmHg at 25°C

[ Index of Refraction ]:
1.575

[ Storage condition ]:
2-8°C


Related Compounds

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