Showing 1-30 of 47 results for "P9053"
A Bayir et al.
Human & experimental toxicology, 32(1), 45-52 (2012-10-13)
The aim of this study was to examine the effects of ubiquinone (CoQ10) on heart tissue and erythrocytes in acute organophosphate poisoning (AOP). A total of 20 rabbits were divided into three groups: sham (n = 8), pralidoxime (PAM) +...
Jyotiranjan Acharya et al.
European journal of medicinal chemistry, 46(9), 3926-3933 (2011-06-28)
A series of carbamoyl bis-pyridinium monooximes linked with xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by organophosphorus inhibitors (OP) such as sarin, DFP and VX and the data were compared with reactivation...
Amitraz poisoning -- familiar presentation, unfamiliar diagnosis.
B Batra et al.
Anaesthesia and intensive care, 40(2), 363-364 (2012-03-16)
Kamil Musilek et al.
Journal of medicinal chemistry, 50(22), 5514-5518 (2007-10-11)
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Among the organophosphates, with the exception of soman, tabun (GA) intoxications are the least responsive to treatment with commercially available therapeutics. A rational design was used to increase reactivation...
Nadir Chabane et al.
Journal of cellular biochemistry, 106(3), 453-463 (2008-12-31)
Microsomal prostaglandin E synthase-1 (mPGES-1) catalyzes the terminal step in the biosynthesis of PGE(2), which contributes to many physiopathological processes. We show here that inhibitors of histone deacetylase (HDAC) activity, trichostatin A (TSA), butyric acid (BA), and valproic acid (BA)...
Enes Elvin Gul et al.
Cardiovascular toxicology, 12(3), 263-265 (2012-04-25)
Organophosphate pesticides have emerged as a common cause of poisoning, particularly in developing countries. The most common electrocardiographic abnormalities observed in organophosphate poisoning are sinus tachycardia, QT interval prolongation, and, very rarely, ventricular arrhythmias. We report a case of organophosphate...
Kamil Musilek et al.
Bioorganic & medicinal chemistry, 16(17), 8218-8223 (2008-08-05)
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and...
Harald John et al.
Drug testing and analysis, 4(3-4), 179-193 (2011-09-29)
Pralidoxime (2-PAM) belongs to the class of monopyridinium oximes with reactivating potency on cholinesterases inhibited by phosphylating organophosphorus compounds (OPC), for example, pesticides and nerve agents. 2-PAM represents an established antidote for the therapy of anticholinesterase poisoning since the late...
Diabetic ketoacidosis: an uncommon manifestation of pesticide poisoning.
Krishnan Swaminathan et al.
Diabetes care, 36(1), e4-e4 (2012-12-25)
Hee Chun Jeong et al.
Bioorganic & medicinal chemistry, 17(17), 6213-6217 (2009-08-12)
A series of fluorinated oxime compounds was designed and synthesized in order to probe the effect of fluorine substitution on reactivation of inhibited acetylcholinesterase (AChE) by organophosphorus agents. Permeability measurements, using the Parallel Artificial Membrane Permeation Assays (PAMPA) method, were...
Kamil Musilek et al.
Bioorganic & medicinal chemistry letters, 16(3), 622-627 (2005-11-18)
Six potential AChE reactivators were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by insecticide chlorpyrifos was tested in vitro. According to the results, (E)-1-(2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide seems to be the most potent AChE reactivator....
Harald John et al.
Drug testing and analysis, 4(3-4), 169-178 (2011-11-22)
Pralidoxime (2-PAM) is a monopyridinium oxime used as an antidote for the treatment of poisoning with organophosphorus (OP) compounds, for example, pesticides and nerve agents, reactivating OP-inhibited acetylcholinesterase. However, appropriate dosing and efficacy remains a matter of discussion requiring experimental...
Kamil Musilek et al.
Bioorganic & medicinal chemistry, 15(21), 6733-6741 (2007-09-04)
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Fifteen new monooxime reactivators of acetylcholinesterase with a (E)-but-2-ene linker were developed in an effort to extend the properties of K-oxime (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). The known reactivators (pralidoxime, HI-6...
Jyotiranjan Acharya et al.
European journal of medicinal chemistry, 44(3), 1326-1330 (2008-04-09)
A series of bis-pyridinium oximes connected by xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by nerve agent, sarin. Among the synthesized compounds, alpha,alpha'xylene-bis-[3,3'-(hydroxyiminomethyl) pyridinium] dibromide (3b) was found to be most potent...
Yusuf Parvez et al.
Indian pediatrics, 49(9), 752-753 (2012-10-02)
Organophosphorus poisoning in neonates is extremely rare and needs high index of suspicion to diagnose it. The clinical presentation is often confused with the features of sepsis like apnea, copious oral secretions, diarrhea, letharginess, seizures. There may be recurrence of...
Misako Yorimitsu et al.
Magnetic resonance in medical sciences : MRMS : an official journal of Japan Society of Magnetic Resonance in Medicine, 11(1), 9-16 (2012-03-28)
Whole-heart 3-dimensional (3D) late-gadolinium-enhanced magnetic resonance (MR) imaging (WH-LGE) uses respiratory gating combined with acquisition of 3D data for the entire heart in a single scan, which permits reconstruction of any plane with high resolution. We investigated the optimal scan...
Chennamaneni Srinivas Rao et al.
Bioorganic & medicinal chemistry letters, 16(8), 2134-2138 (2006-02-17)
In continuation of our investigations of unsymmetrical bisquaternary monooximes, we synthesized four new series of compounds bridged by hexyl, heptyl, octyl and nonyl groups. All eight monooximes viz., dibromides of 1-(4-hydroxyiminomethylpyridinium)6-(3/4-carbamoylpyridinium)hexane, 1-(4-hydroxyiminomethylpyridinium)-7-(3/4-carbamoylpyridinium)heptane, 1-(4-hydroxyiminomethylpyridinium)-8-(3/4-carbamoylpyridinium)octane, 1-(4-hydroxyiminomethylpyridinium)-9-(3/4-carbamoylpyridinium)nonane as well as the corresponding bis-oximes...
Xue Tang et al.
The American journal of emergency medicine, 31(6), 946-949 (2013-05-18)
This study aimed to clarify the efficacy of 2 therapies for patients with severe acute organophosphorus pesticide poisoning, including atropine adverse effects, the length of intensive care unit (ICU) stay, complications, and mortality. A retrospective cohort study of 152 cases...
Hee Chun Jeong et al.
Bioorganic & medicinal chemistry letters, 19(4), 1214-1217 (2009-01-07)
For the purpose of developing new oxime reactivators of acetylcholinesterases (AChE) that have been inhibited by organophosphorus agents, emphasis was given to the finding that the lipophilic nature of fluorinated compounds is responsible for their enhanced transport across the blood...
S Banerjee et al.
Drug research, 63(9), 450-456 (2013-05-02)
In the present study, a simple, precise, specific, fast, accurate and reliable reverse phase high performance liquid chromatographic (RP-HPLC) method has been developed and validated for the simultaneous determination and quantification of eserine and pralidoxime chloride in drugs-in-adhesive matrix type...
Kamil Musilek et al.
Bioorganic & medicinal chemistry letters, 16(21), 5673-5676 (2006-08-29)
Three asymmetrical AChE reactivators with cyano-moiety and propane linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by nerve agent tabun and insecticide paraoxon was tested in vitro and compared to pralidoxime, HI-6...
F Worek et al.
Archives of toxicology, 72(4), 237-243 (1998-05-20)
The treatment of poisoning by highly toxic organophosphorus compounds (nerve agents) is unsatisfactory. Until now, the efficacy of new potential antidotes has primarily been evaluated in animals. However, the extrapolation of these results to humans is hampered by species differences....
Sumika Nagase et al.
Clinica chimica acta; international journal of clinical chemistry, 416, 72-79 (2012-12-01)
Drugs sometimes alter the results of clinical laboratory tests. We examined the effects of pralidoxime (PAM) salts, a medicine used to treat organophosphorus poisoning, on clinical laboratory test results for the first time. The effects of PAM salts on glucose...
A rare case of combined strychnine and propoxur toxicity from a single preparation.
Jeena Jacob et al.
Clinical toxicology (Philadelphia, Pa.), 50(3), 224-224 (2012-02-18)
Baishali Kanjilal et al.
Toxicology mechanisms and methods, 24(7), 488-494 (2014-07-22)
The US military has placed major emphasis on developing therapeutics against nerve agents (NA). Current efforts are hindered by the lack of effective in vitro cellular models to aid in the preliminary screening of potential candidate drugs/antidotes. The development of...
Eichi Narimatsu et al.
The American journal of emergency medicine, 30(6), 901-907 (2011-08-30)
The composite effects of organophosphorus (OP)-cholinesterase (ChE) inhibitors and oximes on the actions of nondepolarizing neuromuscular blockers in acute OP-ChE inhibitor intoxication have not been evaluated in detail. We investigated the effects of paraoxon (Pox) (an OP-ChE inhibitor) and pralidoxime...
A Basher et al.
Clinical toxicology (Philadelphia, Pa.), 51(1), 35-40 (2013-01-15)
Acute organophosphorus (OP) poisoning is relatively common and a major cause of death from poisoning in developing countries. Magnesium has been shown to be of benefit in animal models. We conducted a phase II study of bolus doses of (MgSO4)...
Jyotiranjan Acharya et al.
European journal of medicinal chemistry, 44(3), 1335-1340 (2008-04-09)
A series of novel bis-pyridinium oximes connected by bis-methoxymethyl benzene, 1,4-bis-methoxymethyl (cis)-but-2-ene and 1,4-bis-methoxymethyl but-2-yne linkers were synthesized and their in vitro reactivation efficacy was evaluated against diisopropyl phosphorofluoridate (DFP) inhibited acetylcholinesterase (AChE) and compared with the established antidote 2-PAM...
Jarosław Kalisiak et al.
Journal of medicinal chemistry, 55(1), 465-474 (2011-12-31)
A new class of amidine-oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) was synthesized and tested in vitro and in vivo. Compared with 2-PAM, the most promising cyclic amidine-oxime (i.e., 12e) showed comparable or greater reactivation of OP-inactivated AChE and OP-inactivated...
Kamil Musilek et al.
Bioorganic & medicinal chemistry letters, 17(11), 3172-3176 (2007-03-27)
Six novel AChE reactivators with a (Z)-but-2-ene linker were synthesized using the known synthetic pathways. Their ability to reactivate AChE, which had been previously inhibited by nerve agent tabun or pesticide paraoxon, was tested in vitro and compared to pralidoxime...

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