Dimetridazole

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Chemical Structure| 551-92-8 同义名 : 1,2-二甲基-5-硝基咪唑 ;1,2-Dimethyl-5-nitroimidazole
CAS号 : 551-92-8
货号 : A138709
分子式 : C5H7N3O2
纯度 : 99%
分子量 : 141.128
MDL号 : MFCD00047046
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(354.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Dimetridazole is a nitroimidazole class drug that combats protozoan infections. Dimetridazole achieved higher MIC100 activity than metronidazole against the resistant isolate. The use of dimetridazole as a promising drug-like scaffold for novel therapeutic alternatives against T. vaginalis resistant infections[3]. Dimetridazole was formulated for drinking water medication and as a prolonged-release tablet. To suppress a Trichomonas gallinae infection successfully, medicated drinking water containing dimetridazole (400 mg/L) had to be administered for at least 3 days. After intravenous administration of 20 mg dimetridazole, the drug plasma concentration-time profile fitted a one-compartment open model with a mean half-life of 3.9 h. The absolute bioavailability of the tablet in fasted pigeons was 83.8%. The bioavailability of the tablet administered with food was reduced by 20%[4]. Dimetridazole, either when used alone or in conjunction with oxytetracycline, had a marked effect on ruminal function. Within 6 h of dosing, the ruminal pH fell to below 5, but then returned to pretreatment values over the next 24 - 48h[5]. Dimetridazole at a concentration of 1.0 g/l in drinking water caused mortality in both ducklings and goslings. When given to goslings at a concentration of 0.5 g/l, the drug caused growth depression and nervous signs characterized by excess activity, abnormal head attitudes, and ataxia[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.09mL

1.42mL

0.71mL

35.43mL

7.09mL

3.54mL

70.86mL

14.17mL

7.09mL
参考文献

[1]Griffin RM. Therapeutic and prophylactic activity of dimetridazole against experimentally-transmitted swine dysentery. Vet Rec. 1972 Oct 7;91(15):349-53.

[2]McLoughlin DK, Chute MB. Effect of quinacrine hydrochloride and acriflavine hydrochloride on development and stability of resistance to dimetridazole by Tritrichomonas foetus. J Parasitol. 1969 Apr;55(2):426-8.

[3]Ibáñez-Escribano A, Meneses-Marcel A, Marrero-Ponce Y, et al. A sequential procedure for rapid and accurate identification of putative trichomonacidal agents. J Microbiol Methods. 2014;105:162‐167

[4]Inghelbrecht S, Vermeersch H, Ronsmans S, Remon JP, DeBacker P, Vercruysse J. Pharmacokinetics and anti-trichomonal efficacy of a dimetridazole tablet and water-soluble powder in homing pigeons (Columba livia). J Vet Pharmacol Ther. 1996;19(1):62‐67

[5]Swan GE, Shakespeare A, Mülders MS, Minnaar PP, Naudé TW, Groeneveld HT. The safety of dimetridazole alone and in conjunction with oxytetracycline in Hereford crossbred steers. J S Afr Vet Assoc. 1991;62(2):55‐59

[6]Riddell C. Toxicity of dimetridazole in waterfowl. Avian Dis. 1984;28(4):974‐977