2. Neuronal Signaling
  3. Cholinesterase (ChE)
  4. Trimedoxime dichloride

Trimedoxime dichloride (TMB-4 dichloride) 是一种可穿透血脑屏障的胆碱酯酶 (Cholinesterase) 复能剂。Trimedoxime dichloride 可复活被对氧磷、沙林、塔崩等抑制的胆碱酯酶，恢复乙酰胆碱的分解并减轻胆碱能过度刺激。Trimedoxime dichloride 可降低死亡率、延长存活时间。Trimedoxime dichloride 在大鼠组织中对 AChE 有复活效力。Trimedoxime dichloride 可用于有机磷酸酯 (对氧磷) 中毒和塔崩中毒的相关研究。

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Trimedoxime dichloride

Trimedoxime dichloride Chemical Structure

CAS No. : 3613-82-9

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Other Forms of Trimedoxime dichloride:

Trimedoxime dichloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning[1][2][3].

IC50 & Target[1]

AChE

 

药代动力学
(Parmacokinetics)
Species Dose Route T1/2α T1/2β AUC0-∞ CLtotal Vd V1
Mice[2] 55.98 μM/kg i.v. 8.96 min 108.08 min 74.5867 μM/L·h 0.0125 L/min/kg 1.95 L/kg 0.22 L/kg
体内研究
(In Vivo)

Trimedoxime (25 µM/rat；腹腔注射；单次给药) dichloride 对雄性 Wistar 大鼠的对氧磷诱导死亡具有保护作用[1]。
Trimedoxime (7.5 mg/kg；肌内注射；单次) dichloride 可显著重新活化被塔崩抑制的大鼠血液及膈肌中的乙酰胆碱酯酶 (AChE)，活化率分别为 17.5%和 34.7%，但对大鼠脑内该酶的活化作用极弱 (仅 2.8%)，降低塔崩对小鼠的急性致死作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (male, 200-250 g, organophosphate poisoning model via intraperitoneal paraoxon exposure)[1]
Dosage: 25 µM/rat
Administration: i.p.; single dose
Result: Reduced 48-hour mortality to 38% in rats exposed to 1 µmol/rat paraoxon.
Reduced 48-hour mortality to 76% in rats exposed to 10 µmol/rat paraoxon.
Reduced 48-hour mortality to 83% in rats exposed to 15 µmol/rat paraoxon.
Lowered the relative risk of death to 0.36 (95% confidence interval, 0.26 to 0.50) compared to paraoxon-only controls.
Animal Model: Wistar (male, 180-200 g, tabun poisoning model)[3]
Dosage: 7.5 mg/kg
Administration: i.m.; single prophylactic dose
Result: Produced 17.5% reactivation of tabun-inhibited AChE in blood.
Produced 34.7% reactivation of tabun-inhibited AChE in diaphragm.
Produced 2.8% reactivation of tabun-inhibited AChE in brain.
Showed significant differences from atropine-only control and HI-6 treatment group.
Increased the LD50 of tabun in mice to 504.8 μg/kg.
Resulted in a protective ratio of 1.71.
Showed significant difference from untreated group and HI-6 treatment group.
分子量

357.24

Formula

C15H18Cl2N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Trimedoxime dichloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Trimedoxime dichloride3613-82-9TMB-4 dichlorideCholinesterase (ChE)miceorganophosphate poisoningtabunmale Wistar ratsVXparaoxoncholinesteraseblood-brain barriersarinacetylcholinesteraseInhibitorinhibitorinhibit

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