Trimedoxime dichloride
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.
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- CAS No.: 3613-82-9
- 화학식: C15H18Cl2N4O2
- 분자량:357.24
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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AChE |
| 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 |
Trimedoxime (7.5 mg/kg; i.m.; single dose) dichloride significantly reactivates acetylcholinesterase (AChE) inhibited by tabun in rat blood and diaphragm, with reactivation rates of 17.5% and 34.7%, respectively, but exerts extremely weak reactivation on this enzyme in rat brain (only 2.8%), and reduces the acute lethal effect of tabun in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 200-250 g, organophosphate poisoning model via intraperitoneal paraoxon exposure)[1]
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Dosage:25 µM/rat
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Administration:i.p.; single dose
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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.
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Animal Model:Wistar (male, 180-200 g, tabun poisoning model)[3]
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Dosage:7.5 mg/kg
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Administration:i.m.; single prophylactic dose
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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.
Chemical Information
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CAS No. 3613-82-9
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분자량 357.24
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화학식 C15H18Cl2N4O2
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SMILES
O/N=C/C1=CC=[N+](CCC[N+]2=CC=C(C=C2)/C=N/O)C=C1.[Cl-].[Cl-]
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Synonyms
TMB-4 dichloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Petroianu GA, et al. New K-Oximes (K-27 and K-48) in Comparison with Obidoxime (LuH-6), HI-6, Trimedoxime (TMB-4), and Pralidoxime (2-PAM): Survival in Rats Exposed IP to the Organophosphate Paraoxon. Toxicol Mech Methods. 2007;17(7):401-8. [Content Brief]
[2]. Milic B, et al. Trimedoxime and HI-6: kinetic comparison after intravenous administration to mice. Pharmacol Toxicol. 1996;78(4):269-272. [Content Brief]
[3]. Kassa J, et al. An evaluation of therapeutic and reactivating effects of newly developed oximes (K156, K203) and commonly used oximes (obidoxime, trimedoxime, HI-6) in tabun-poisoned rats and mice. Toxicology. 2008;243(3):311-316. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trimedoxime dichloride Related Classifications
HY-165600 Related Classifications
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