Obidoxime dichloride
(Synonyms: 双复磷) 目录号 : GC63305
An AChE modulator
Cas No.:114-90-9
Sample solution is provided at 25 µL, 10mM.
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Obidoxime is an acetylcholinesterase (AChE) modulator.1 It induces inhibition and activation of bovine erythrocyte AChE in the presence and absence of ACh, respectively, when used at a concentration of 3 mM. Obidoxime (10.5 mg/kg) induces reactivation of tabun-inhibited AChE in rat blood and diaphragm and reduces tabun-induced lethality in mice.2 Intranasal administration of obidoxime reduces seizure duration and severity and prevents mortality in a rat model of paraoxon-induced organophosphate poisoning.3
1.Kuhnen, H.Activating and inhibitory effects of bispyridinium compounds on bovine red cell acetylcholinesteraseToxicol. Appl. Pharmacol.20(1)97-104(1971) 2.Kassa, J., Karasova, J., Musilek, K., 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 miceToxicology243(3)311-316(2008) 3.Krishnan, J.K.S., Arun, P., Appu, A.P., et al.Intranasal delivery of obidoxime to the brain prevents mortality and CNS damage from organophosphate poisoningNeurotoxicology5364-73(2016)
Cas No. | 114-90-9 | SDF | |
别名 | 双复磷 | ||
分子式 | C14H16Cl2N4O3 | 分子量 | 359.21 |
溶解度 | 储存条件 | Store at -20°C | |
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1 mg | 5 mg | 10 mg |
1 mM | 2.7839 mL | 13.9194 mL | 27.8389 mL |
5 mM | 0.5568 mL | 2.7839 mL | 5.5678 mL |
10 mM | 0.2784 mL | 1.3919 mL | 2.7839 mL |
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Efficacy of pralidoxime iodide and Obidoxime dichloride as antidotes in diazinon-poisoned goslings
Avian Dis 1976 Jan-Mar;20(1):162-6.PMID:769769doi
The antidotal efficacy of pralidoxime iodide and Obidoxime dichloride was investigated in goslings poisoned by a supralethal dose of the organophosphorus insecticide diazinon. Various doses of both drugs were administered by intramuscular injection when the poisoned birds were unable to walk. Pralidoxime at 100 mg/kg brought about a complete and speedy clinical recovery. Fifty mg/kg induced recovery in 4 of 6 poisoned goslings, and 25 mg/kg successfully trated only 1 of 6 birds. Obidoxime at 25 mg/kg showed no therapeutic properties whereas 50 and 100 mg/kg delayed the death of some birds by several hours. At 100 mg/kg, all goslings had transient signs of intoxication, which precluded the use of this compound as an antidote at higher doses. The mode of action of these antidotes in diazinon-poisoned goslings is discussed.
Nanoparticulate transport of oximes over an in vitro blood-brain barrier model
PLoS One 2010 Dec 3;5(12):e14213.PMID:21151975DOI:10.1371/journal.pone.0014213.
Background: Due to the use of organophosphates (OP) as pesticides and the availability of OP-type nerve agents, an effective medical treatment for OP poisonings is still a challenging problem. The acute toxicity of an OP poisoning is mainly due to the inhibition of acetylcholinesterase (AChE) in the peripheral and central nervous systems (CNS). This results in an increase in the synaptic concentration of the neurotransmitter acetylcholine, overstimulation of cholinergic receptors and disorder of numerous body functions up to death. The standard treatment of OP poisoning includes a combination of a muscarinic antagonist and an AChE reactivator (oxime). However, these oximes can not cross the blood-brain barrier (BBB) sufficiently. Therefore, new strategies are needed to transport oximes over the BBB. Methodology/principal findings: In this study, we combined different oximes (Obidoxime dichloride and two different HI 6 salts, HI 6 dichloride monohydrate and HI 6 dimethanesulfonate) with human serum albumin nanoparticles and could show an oxime transport over an in vitro BBB model. In general, the nanoparticulate transported oximes achieved a better reactivation of OP-inhibited AChE than free oximes. Conclusions/significance: With these nanoparticles, for the first time, a tool exists that could enable a transport of oximes over the BBB. This is very important for survival after severe OP intoxication. Therefore, these nanoparticulate formulations are promising formulations for the treatment of the peripheral and the CNS after OP poisoning.
Assessing the therapeutic efficacy of oxime therapies against percutaneous organophosphorus pesticide and nerve agent challenges in the Hartley guinea pig
J Toxicol Sci 2015 Dec;40(6):759-75.PMID:26558457DOI:10.2131/jts.40.759.
Given the rapid onset of symptoms from intoxication by organophosphate (OP) compounds, a quick-acting, efficacious therapeutic regimen is needed. A primary component of anti-OP therapy is an oxime reactivator to rescue OP-inhibited acetylcholinesterases. Male guinea pigs, clipped of hair, received neat applications of either VR, VX, parathion, or phorate oxon (PHO) at the 85(th) percentile lethal dose, and, beginning with presentation of toxicosis, received the human equivalent dose therapy by intramuscular injection with two additional follow-on treatments at 3-hr intervals. Each therapy consisted of atropine free base at 0.4 mg/kg followed by one of eight candidate oximes. Lethality rates were obtained at 24 hr after VR, VX and PHO challenges, and at 48 hr after challenge with parathion. Lethality rates among symptomatic, oxime-treated groups were compared with that of positive control (OP-challenged and atropine-only treated) guinea pigs composited across the test days. Significant (p ≤ 0.05) protective therapy was afforded by 1,1-methylene bis(4(hydroxyimino- methyl)pyridinium) dimethanesulfonate (MMB4 DMS) against challenges of VR (p ≤ 0.001) and VX (p ≤ 0.05). Lethal effects of VX were also significantly (p ≤ 0.05) mitigated by treatments with oxo-[[1-[[4-(oxoazaniumylmethylidene)pyridin-1-yl]methoxymethyl]pyridin-4-ylidene]methyl]azanium dichloride (obidoxime Cl2) and 1-(((4-(aminocarbonyl) pyridinio)methoxy)methyl)-2,4-bis((hydroxyimino)methyl)pyridinium dimethanesulfonate (HLö-7 DMS). Against parathion, significant protective therapy was afforded by Obidoxime dichloride (p ≤ 0.001) and 1,1'-propane-1,3-diylbis{4-[(E)-(hydroxyimino)methyl]pyridinium} dibromide (TMB-4, p ≤ 0.01). None of the oximes evaluated was therapeutically effective against PHO. Across the spectrum of OP chemicals tested, the oximes that offered the highest level of therapy were MMB4 DMS and Obidoxime dichloride.