Cholinesterase Reactivators
Obidoxime Chloride
Cholinesterase Inhibitors
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
Oximes
Pralidoxime Compounds
Various salts of a quaternary ammonium oxime that reconstitute inactivated acetylcholinesterase, especially at the neuromuscular junction, and may cause neuromuscular blockade. They are used as antidotes to organophosphorus poisoning as chlorides, iodides, methanesulfonates (mesylates), or other salts.
Acetylcholinesterase
Sarin
Organophosphates
Carbon-containing phosphoric acid derivatives. Included under this heading are compounds that have CARBON atoms bound to one or more OXYGEN atoms of the P(=O)(O)3 structure. Note that several specific classes of endogenous phosphorus-containing compounds such as NUCLEOTIDES; PHOSPHOLIPIDS; and PHOSPHOPROTEINS are listed elsewhere.
Chemical Warfare Agents
Organophosphate Poisoning
Organophosphorus Compounds
Enzyme Reactivators
Thiocholine
Trichlorfon
Phenylcarbamates
Chlorpyrifos
Neostigmine
Dibucaine
Tacrine
Physostigmine
Galantamine
A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.
Tetraisopropylpyrophosphamide
Insecticides
Parathion
Organothiophosphorus Compounds
Succinylcholine
A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.
Pyridostigmine Bromide
Carbaryl
Carbamates
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
Butyrylthiocholine
Bacteriology
Ophthalmology
Encyclopedias as Topic
Buttocks
Drug Delivery Systems
A case of aldicarb poisoning: a possible murder attempt. (1/98)
A couple showing signs of cholinergic crisis was admitted to the hospital. Analyses with high-performance liquid chromatography and gas chromatography-mass spectrometry conducted on serum, urine, and stomach contents that were collected few hours after first symptoms showed the presence of aldicarb, which is the most potent carbamate insecticide on the market. A murder attempt was suspected because the patients showed the first signs some minutes after drinking coffee upon returning home and no commercial products containing aldicarb were found in the house. Because of the reversibility of inhibition of acetylcholinesterase, the patients recovered after treatment with atropine and toxogonin. They left the hospital after 12 days. To our knowledge, the serum concentrations of aldicarb reported in this paper are the highest reported for a nonfatal case. (+info)Positive inotropic effect of insulin-like growth factor-1 on normal and failing cardiac myocytes. (2/98)
OBJECTIVE: The acute administration of growth hormone (GH) or insulin-like growth factor-1 (IGF-1) improves cardiac performance, possibly contributing to the beneficial effects of GH therapy on heart failure (HF). GH can induce the production of IGF-1 and thus the actions of GH may be mediated through its IGF-1 induction. However, these effects have not yet been demonstrated in failing hearts and the cellular basis of GH or IGF-1-induced inotropic effects remains unknown. We examined the direct effects of GH and IGF-1 on the contractile function and intracellular calcium ([Ca2+]i) homeostasis in normal and failing myocytes. METHODS: To determine whether GH and IGF-1 have a direct effect on myocardial contractility and whether the GH/IGF-1-induced effect was the results of changes in Ca2+ activation, cell shortening and [Ca2+]i transient were simultaneously measured in the left ventricular myocyte preparations, isolated from normal and rapid pacing-induced HF dogs. RESULTS: Basal shortening of HF myocytes was reduced by 64% (p < 0.01). In normal and HF myocytes, GH (0.4-40 x 10(-3) IU/ml) had no effect on either cell shortening or [Ca2+]i transients. In normal myocytes, IGF-1 exerted a positive inotropic effect in a time- and dose-dependent manner (25-500 ng/ml), associated with a parallel increase of [Ca2+]i transient amplitude. IGF-1 increased the shortening magnitude in normal (121 +/- 5% increase from baseline, p < 0.05) and HF (118 +/- 4% increase from baseline, p < 0.05) myocytes. It also increased [Ca2+]i transient amplitude in normal and HF cells by 124 +/- 4 and 125 +/- 7%, respectively. The percent increase of cell shortening and [Ca2+]i transient amplitude was comparable between normal and HF myocytes. Furthermore, IGF-1 did not shift the trajectory of the relaxation phase in the phase-plane plots of cell length vs. [Ca2+]i, indicating that it did not change myofilament Ca2+ sensitivity. CONCLUSIONS: In both normal and HF conditions, IGF-1 exerted an acute direct positive inotropic effect in adult cardiac myocytes by increasing the availability of [Ca2+]i to the myofilaments, possibly explaining the beneficial effect of GH on HF. (+info)Inhibitory effect of 2,3-butanedione monoxime (BDM) on Na(+)/Ca(2+) exchange current in guinea-pig cardiac ventricular myocytes. (3/98)
1. The effect of 2,3-butanedione monoxime (BDM), a 'chemical phosphatase', on Na(+)/Ca(2+) exchange current (I(NCX)) was investigated using the whole-cell voltage-clamp technique in single guinea-pig cardiac ventricular myocytes and in CCL39 fibroblast cells expressing canine NCX1. 2. I(NCX) was identified as a current sensitive to KB-R7943, a relatively selective NCX inhibitor, at 140 mM Na(+) and 2 mM Ca(2+) in the external solution and 20 mM Na(+) and 433 nM free Ca(2+) in the pipette solution. 3. In guinea-pig ventricular cells, BDM inhibited I(NCX) in a concentration-dependent manner. The IC(50) value was 2.4 mM with a Hill coefficients of 1. The average time for 50% inhibition by 10 mM BDM was 124+/-31 s (n=5). 4. The effect of BDM was not affected by 1 microM okadaic acid in the pipette solution, indicating that the inhibition was not via activation of okadaic acid-sensitive protein phosphatases. 5. Intracellular trypsin treatment via the pipette solution significantly suppressed the inhibitory effect of BDM, implicating an intracellular site of action of BDM. 6. PAM (pralidoxime), another oxime compound, also inhibited I(NCX) in a manner similar to BDM. 7. Isoprenaline at 50 microM and phorbol 12-myristate 13-acetate (PMA) at 8 microM did not reverse the inhibition of I(NCX) by BDM. 8. BDM inhibited I(NCX) in CCL39 cells expressing NCX1 and in its mutant in which its three major phosphorylatable serine residues were replaced with alanines. 9. We conclude that BDM inhibits I(NCX) but the mechanism of inhibition is not by dephosphorylation of the Na(+)/Ca(2+) exchanger as a 'chemical phosphatase'. (+info)Force spectroscopy between acetylcholine and single acetylcholinesterase molecules and the effects of inhibitors and reactivators studied by atomic force microscopy. (4/98)
Force spectroscopy between a single acetylcholinesterase (AChE) molecule and its natural substrates was performed, and the effects of inhibitors and reactivators on the force spectrum were studied with atomic force microscopy (AFM). The force spectrum between normal AChE and its substrates had its special shape. Inhibitors, which inhibit AChE by occupying the active center of the enzyme, could change the force spectrum shape noticeably. Reactivators, which reactivate the inhibited AChE by pulling the inhibitor off the active center of the enzyme, could make the normal shape of force spectrum reappear. This meant the shape features of the force spectrum could be used as a good index to observe the time course of the interactions between a single AChE molecule and its special inhibitors and reactivators in real time. The results of the real-time observation demonstrated that the inhibition times of soman and sarin on AChE were longer than 2 h and that of eserine, a reversible inhibitor of AChE, was 34 +/- 3 min. The reactivation time of HI-6 on soman-inhibited AChE was 6 +/- 2 min. These results indicated that AFM was a useful tool in pharmacology and toxicology, and could reveal time information of the interactions between AChE and its ligands. (+info)Cholinesterase inhibition by aluminium phosphide poisoning in rats and effects of atropine and pralidoxime chloride. (5/98)
AIM: To investigate the cholinesterase inhibition and effect of atropine and pralidoxime (PAM) treatment on the survival time in the rat model of aluminium phosphide (AlP) poisoning. METHODS: The rats were treated with AlP (10 mg/kg; 5.55 x LD50; ig) and the survival time was noted. The effect of atropine (1 mg/kg, ip) and PAM (5 mg/kg, ip) was noted on the above. Atropine and PAM were administered 5 min after AlP. Plasma cholinesterase levels were measured spectrophotometrically in the control and AlP treated rats 30 min after administration. RESULTS: Treatment with atropine and PAM increased the survival time by 2.5 fold (1.4 h+/-0.3 h vs 3.4 h+/-2.5 h, P < 0.01) in 9 out of 15 animals and resulted in total survival of the 6 remaining animals. Plasma cholinesterase levels were inhibited by 47 %, (438+/-74) U/L in AlP treated rats as compared to control (840+/-90) U/L (P < 0.01). CONCLUSION: This preliminary study concludes that AlP poisoning causes cholinesterase inhibition and responds to treatment with atropine and PAM. (+info)Reactivation of immobilized acetyl cholinesterase in an amperometric biosensor for organophosphorus pesticide. (6/98)
Biosensors based on acetyl cholinesterase (AChE) inhibition have been known for monitoring of pesticides in food and water samples. However, strong inhibition of the enzyme is a major drawback in practical application of the biosensor which can be overcome by reactivation of the enzyme for repeated use. In the present study, enzyme reactivation by oximes was explored for this purpose. Two oximes viz., 1,1'-trimethylene bis 4-formylpyridinium bromide dioxime (TMB-4) and pyridine 2-aldoxime methiodide (2-PAM) were compared for the reactivation of the immobilized AChE. TMB-4 was found to be a more efficient reactivator under repeated use, retaining more than 60% of initial activity after 11 reuses, whereas in the case of 2-PAM, the activity retention dropped to less than 50% after only 6 reuses. Investigations also showed that reactivation must be effected within 10 min after each analysis to eliminate the ageing effect, which reduces the efficiency of reactivation. (+info)Myosin II is present in gastric parietal cells and required for lamellipodial dynamics associated with cell activation. (7/98)
Nonmuscle myosin II has been shown to participate in organizing the actin cytoskeleton in polarized epithelial cells. Vectorial acid secretion in cultured parietal cells involves translocation of proton pumps from cytoplasmic vesicular membranes to the apical plasma membrane vacuole with coordinated lamellipodial dynamics at the basolateral membrane. Here we identify nonmuscle myosin II in rabbit gastric parietal cells. Western blots with isoform-specific antibodies indicate that myosin IIA is present in both cytosolic and particulate membrane fractions whereas the IIB isoform is associated only with particulate fractions. Immunofluorescent staining demonstrates that myosin IIA is diffusely located throughout the cytoplasm of resting parietal cells. However, after stimulation, myosin IIA is rapidly redistributed to lamellipodial extensions at the cell periphery; virtually all the cytoplasmic myosin IIA joins the newly formed basolateral membrane extensions. 2,3-Butanedione monoximine (BDM), a myosin-ATPase inhibitor, greatly diminishes the lamellipodial dynamics elicited by stimulation and retains the pattern of myosin IIA cytoplasmic staining. However, BDM had no apparent effect on the stimulation associated redistribution of H,K-ATPase from a cytoplasmic membrane compartment to apical membrane vacuoles. The myosin light chain kinase inhibitor 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine (ML-7) also did not alter the stimulation-associated recruitment of H,K-ATPase to apical membrane vacuoles, but unlike BDM it had relatively minor inhibitory effects on lamellipodial dynamics. We conclude that specific disruption of the basolateral actomyosin cytoskeleton has no demonstrable effect on recruitment of H,K-ATPase-rich vesicles into the apical secretory membrane. However, myosin II plays an important role in regulating lamellipodial dynamics and cortical actomyosin associated with parietal cell activation. (+info)Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. (8/98)
To improve the potency of 2-pralidoxime (2-PAM) for treating organophosphate poisoning, we dimerized 2-PAM and its analogs according to Wilson's pioneering work and the 3D structure of human acetylcholinesterase (hAChE) inactivated by isoflurophate. 1,7-Heptylene-bis-N,N'-syn-2-pyridiniumaldoxime, the most potent of the alkylene-linked dimeric reactivators, was readily synthesized using bistriflate and is 100 times more potent than 2-PAM in reactivating hAChE poisoned by isoflurophate. Experimental and computational studies confirm that 2-PAM in its biologically active form adopts the syn-I configuration. Further, they suggest that the improved performance of dimeric oximes is conferred by two-site binding with one oxime pointing toward the diisopropyl ester at the catalytic site of hAChE and the other anchored at the peripheral site. This type of binding may induce a conformational change in the acyl pocket loop which modulates the catalytic site via a domino effect. (+info)
From Pyridinium-based to Centrally Active Acetylcholinesterase Reactivators | BenthamScience
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ATNAA
V. The effect of oximes and related cholinesterase reactivators. Teratology 15: 33 (Feb) 1977. Moller, K.O., Jensen-Holm, J. ...
Organophosphate poisoning
2015 Jokanović M, Prostran M (2009). "Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and ... Significant advances with cholinesterases (ChEs), specifically human serum BChE (HuBChE) have been made. HuBChe can offer a ... "Cholinesterase Inhibition". Archived from the original on 2013-04-02. "Pesticide Application and Safety Training for ... He was later transferred to Berlin, where poisoning by a cholinesterase inhibitor was diagnosed and confirmed by multiple tests ...
Pralidoxime
Jokanović M, Prostran M (2009). "Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and efficacy ... "Current understanding of the application of pyridinium oximes as cholinesterase reactivators in treatment of organophosphate ...
Obidoxime
Jokanović M, Prostran M (2009). "Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and efficacy ...
Tetraethyl pyrophosphate
Petroianu, Georg (2015). "History of organophosphorus cholinesterase inhibitors & reactivators". Military Medical Science ... Historical development of organophosphorus cholinesterase inhibitors." Handbook of Experimental Pharmacology.". Cholinesterases ... doi:10.1007/978-3-642-68441-8. ISBN 978-3-642-68443-2.The history of cholinesterase inhibitors: who was Moschnin(e)? "9: " ... TEPP was discovered to be an inhibitor of cholinesterases. Schrader referred to the studies by Eberhard Gross, who was the ...
Dimethylheptylpyran
2: Cholinesterase Reactivators, Psychochemicals and Irritants and Vesicants. Commission on Life Sciences. The National ...
Edgewood Arsenal human experiments
Similarly, cholinesterase reactivators antidotes such as 2-PAM were tested on about 750 subjects. These agents are still used ... 2, "Cholinesterase Reactivators, Psychochemicals and Irritants and Vesicants" (1984) Vol. 3, "Final Report: Current Health ... 2, "Cholinesterase Reactivators, Psychochemicals and Irritants and Vesicants (1984) Vol. 3, "Final Report: Current Health ... 2, "Cholinesterase Reactivators, Psychochemicals and Irritants and Vesicants (1984) Vol. 3, "Final Report: Current Health ...
Chlorfenvinphos
Administration of a cholinesterase reactivator, in the pyridinium oxime family, usually pralidoxime; Administration of ... However, cholinesterase inhibition is caused by all anticholinesterase compounds and is therefore not a specific biomarker for ... Two pools of cholinesterases exist in the blood: acetylcholinesterase in erythrocytes and pseudocholinesterase in plasma. The ... In addition, the activity of cholinesterases in the blood varies in populations and there are no studies which have measured a ...
3-Quinuclidinyl benzilate
Possible Long-Term Health Effects of Short-Term Exposure To Chemical Agents, Volume 2: Cholinesterase Reactivators, ...
THC-O-acetate
Cholinesterase Reactivators, Psychochemicals and Irritants and Vesicants. The National Academies Press. p. 79. ISBN 978-0-309- ...
List of MeSH codes (D27)
... enzyme reactivators MeSH D27.505.519.405.347 - cholinesterase reactivators MeSH D27.505.519.421 - fibrin modulating agents MeSH ... cholinesterase inhibitors MeSH D27.505.519.625.120.400 - cholinesterase reactivators MeSH D27.505.519.625.150 - dopamine agents ... cholinesterase inhibitors MeSH D27.505.696.577.120.400 - cholinesterase reactivators MeSH D27.505.696.577.150 - dopamine agents ... cholinesterase inhibitors MeSH D27.505.519.389.310 - cyclooxygenase inhibitors MeSH D27.505.519.389.310.500 - cyclooxygenase 2 ...
Soman
... can also bind to other esterases, e.g., AChE, cholinesterase (ChE) and carboxylesterases (CarbE). In this binding, soman ... oxime reactivators. The rate of this process is dependent on the OP. Soman is an OP that stimulates the rate of aging most ... interfering with normal functioning of the mammalian nervous system by inhibiting the enzyme cholinesterase. It is an inhibitor ... "Behavioral Changes in the Rat after Low Doses of Cholinesterase Inhibitors". Toxicological Sciences. 4 (2part2): 195-208. doi: ...
Methylfluorophosphonylcholine
MFPCh is resistant to oxime reactivators, meaning the acetylcholinesterase inhibited by MFPCh can't be reactivated by oxime ... "Experiments with Methyl-fluoro-phosphorylcholine-inhibited Cholinesterase". Acta Chemica Scandinavica. 12: 780-781. doi:10.3891 ... reactivators. MFPCh also acts directly on the acetylcholine receptors. However, despite its high toxicity, ...
Schradan
... , named after Gerhard Schrader, is an obsolete organophosphate insecticide.[1] Schradan itself is a weak cholinesterase ... "The conversion of schra dan (OMPA) and parathion into inhibitors of cholinesterase by mammalian liver". The Biochemical ...
Huperzine A
"Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine". Acta Pharmacologica ...
Acetylcholinesterase inhibitor
An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical or a drug that inhibits the ... Some major effects of cholinesterase inhibitors: *Actions on the parasympathetic nervous system, (the parasympathetic branch of ... Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have ... Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical ...
Donepezil
... , like other cholinesterase inhibitors, can cause nightmares due to enhanced activation of the visual association ... Donepezil along with other cholinesterase inhibitors is suggested as having potential for trouble behaviors, irritability, ... Donepezil binds and reversibly inactivates the cholinesterases, thus inhibiting hydrolysis of acetylcholine. This increases ...
Neuromuscular-blocking drug
For similar term named Cholinesterase-blocking drug, see Cholinesterase inhibitor.. Neuromuscular-blocking drugs block ... Also, they protect the molecule from hydrolysis by cholinesterases, which explain its nature of kidney excretion. The four ... because of hydrolysis by various cholinesterases (such as butyrylcholinesterase in the blood). Succinylcholine was originally ...
Anticholinergic
Not to be confused with Anti-cholinesterase.. Chemical substance that blocks the neurotransmitter acetylcholine in the central ...
cholinesterase reactivators
... Summary. Summary: Drugs used to reverse the inactivation of cholinesterase caused by ... Oximes are cholinesterase reactivators of use in poisoning with organophosphorus ester enzyme inhibitors. Pralidoxime (PRX) is ... PAM-2), trimedoxime (TMB-4), obidoxime (LüH-6, Toxogonin), HI-6 and HLö-7 which are used as cholinesterase reactivators in the ... Oximes are cholinesterase reactivators used in organophosphorus poisoning. Clinical experience with pralidoxime (PRX) and other ...
DailyMed - Search Results for Cholinesterase Reactivator
A noncholinesterase component in the molecular mechanism of action of the cholinesterase reactivator dipyroxime | SpringerLink
3. Psychochemicals | Possible Long-Term Health Effects of Short-Term Exposure To Chemical Agents, Volume 2: Cholinesterase...
Previous: 2. Cholinesterase Reactivators Page 47 Share Cite Suggested Citation:"3. Psychochemicals." National Research Council ... Possible Long-Term Health Effects of Short-Term Exposure To Chemical Agents, Volume 2: Cholinesterase Reactivators, ... Possible Long-Term Health Effects of Short-Term Exposure To Chemical Agents, Volume 2: Cholinesterase Reactivators, ... Possible Long-Term Health Effects of Short-Term Exposure To Chemical Agents, Volume 2: Cholinesterase Reactivators, ...
Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A...
Title:Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A ... Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A ... Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A ... "Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A ...
Pralidoxime
-
Antidotes, Cholinesterase Reactivators, ATC:V03AB04
Drug-induced ocular side effects (Book, 2001) [WorldCat.org]
Study to Know the Efficacy of Higher Doses of Pralidoxime in Patients of Organophpsphorus Poisoning. - Full Text View -...
New structural scaffolds for centrally acting oxime reactivators of phosphylated cholinesterases<...
N2 - We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that contain ... AB - We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that contain ... We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that contain ... abstract = "We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that ...
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ATNAA - Wikipedia
Organophosphate poisoning - Wikipedia
2015 Jokanović M, Prostran M (2009). "Pyridinium oximes as cholinesterase reactivators. Structure-activity relationship and ... Significant advances with cholinesterases (ChEs), specifically human serum BChE (HuBChE) have been made. HuBChe can offer a ... "Cholinesterase Inhibition". Archived from the original on 2013-04-02. "Pesticide Application and Safety Training for ... He was later transferred to Berlin, where poisoning by a cholinesterase inhibitor was diagnosed and confirmed by multiple tests ...
Pralidoxime - Wikipedia
Pralidoxime | definition of pralidoxime by Medical dictionary
pral·i·dox·ime/ (pral″ĭ-doks´ēm) a cholinesterase reactivator, used as the chloride salt as an antidote in the treatment of ... a cholinesterase reactivator whose salts are used in treatment of organophosphorus compound poisoning; it also has limited ... Pharmacologic: cholinesterase reactivators. Pregnancy Category: C. Indications. Early (first 24-36 hr) treatment of ... a cholinesterase reactivator, effective against the nicotinic cholinergic effects of organophosphorus compounds; it also has ...
Free USMLE Flashcards about ANS Pharmacology
List the covered cholinesterase reactivators. pralidoxime.. List the indirect reversible cholinesterase inhibitors. donepezil, ... List the cholinesterase reactivators. pralidoxime. Drug that can increase the outflow of aqueous humor by topical aplication, ... A monoquaternary oxime that is a cholinesterase reactivator used in cases of organophosphate poisoning (insecticide). Though it ... List the indirect irreversible cholinesterase inhibitors.. Organophosphates (parathion, others). ...
Molecules | Free Full-Text | Why is Aged Acetylcholinesterase So Difficult to Reactivate? | HTML
Jodanović, M.; Prostran, M. Pyridinium oximes as cholinesterase reactivator. Structure-activity relationship and efficacy in ... reactivator design, and reactivator mechanism that experimenters can harness to produce agents that can covalently modify aged ... Accumulation of tetrahedral intermediates in cholinesterase catalysis: A secondary isotope effect study. J. Am. Chem. Soc. 2010 ... have shown by measurements of β-deuterium secondary isotope effects on kcat that for the deacylation stage of cholinesterase ...
PDB 5fpq structure summary ‹ Protein Data Bank in Europe (PDBe) ‹ EMBL-EBI
PRALIDOXIME CHLORIDE INJECTION (AUTO-INJECTOR)
Pralidoxime chloride is a cholinesterase reactivator.. The principal action of pralidoxime is to reactivate cholinesterase ( ... Pralidoxime chloride is a cholinesterase reactivator.. Chemical Name: 2-formyl-1 methylpyridinium chloride oxime (pyridine-2- ... It has been reported that the supplemental use of oxime cholinesterase reactivators (such as pralidoxime) reduces the incidence ... V. The effect of oximes and related cholinesterase reactivators, Teratology 15:33 (Feb.) 1977. ...
Toxicology L 11-12 Flashcards - Pharmacology Fall 2015 | Brainscape
Protopam | definition of Protopam by Medical dictionary
a cholinesterase reactivator whose salts are used in treatment of organophosphorus compound poisoning; it also has limited ... Pharmacologic: cholinesterase reactivators. Pregnancy Category: C. Indications. Early (first 24-36 hr) treatment of ... value in counteracting overdosage of carbamate-type cholinesterase inhibitors in persons being treated for myasthenia gravis. ...
Masson P[au] - PubMed - NCBI
Cholinesterase reactivators and bioscavengers for pre- and post-exposure treatments of organophosphorus poisoning. ... Optimization of Cholinesterase-Based Catalytic Bioscavengers Against Organophosphorus Agents.. Lushchekina SV, Schopfer LM, ... Mixed cationic liposomes for brain delivery of drugs by the intranasal route: The acetylcholinesterase reactivator 2-PAM as ... Time-course of human cholinesterases-catalyzed competing substrate kinetics.. Mukhametgalieva AR, Aglyamova AR, Lushchekina SV ...
Molecules | Free Full-Text | Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase...
Their reactivation activity was compared with standard reactivators-pralidoxime, obidoxime and HI-6-which are clinically used ... Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, ... Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, ... Their reactivation activity was compared with standard reactivators-pralidoxime, obidoxime and HI-6-which are clinically used ...
Medicine/First Aid/Materials - Wikiversity
Immunodetection of Serum Albumin Adducts as Biomarkers for Organophosphorus Exposure | Journal of Pharmacology and Experimental...
2012) Nonquaternary reactivators for organophosphate-inhibited cholinesterases. J Med Chem 55:465-474. ... Cholinesterase Activity Inhibition by GD Model Compound.. One of the acute toxic effects of nerve agents is the cholinesterase ... Therefore, cholinesterase functional activity can be used as a biomarker in OP poisoning in the short term, but cholinesterase ... Cholinesterase functional activity was detected by the Ellman assay (Ellman et al., 1961). Typically, 20 μl of plasma was used ...
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Current Medicinal Chemistry | Bentham Science
Evaluation of the Influence of Three Newly Developed Bispyridinium Anti‐nicotinic Compounds (MB408, MB442, MB444) on the...
Pyridinium oximes as cholinesterase reactivators. Structure‐activity relationship and efficacy in the treatment of poisoning ... Development and structural modifications of cholinesterase reactivators against chemical warfare agents in last decade: a ... Acetylcholinesterase reactivators modify the functional properties of the nicotinic acetylcholine receptor ion channel ... Comparison of several oximes on reactivation of soman‐induced blood, brain and tissue cholinesterase activity in rats ...
PROTOPAM INJECTION Dosage & Rx Info | Uses, Side Effects
AcetylcholinesteraseOximes as cholinesterase reactivatorsInhibitorsAntidotesAtropineInhibitorAChEOxime reactivatorsOrganophosphatesAldoxime cholinesterase reactivatorsOrganophosphatePralidoxime chlorideAnti-cholinesterase activityIrritants and VesicantsSeverityReactivationInhibitionOrganophosphorusConjugatesInsecticidesStructuralReactivatesBroad-spectrumSubstrateIntoxicationActivityNerve agentInfusionPotentCompoundsMolecularModificationExposureNeutralBloodHours
Acetylcholinesterase10
- First principles calculations of thermodynamics and kinetic parameters and molecular dynamics simulations of acetylcholinesterase reactivators: can mouse data provide new insights into humans? (labome.org)
- Musilek K, Jun D, Cabal J, Kassa J, Gunn Moore F, Kuca K. Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). (labome.org)
- Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. (labome.org)
- If given within 24 hours,after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase. (hmdb.ca)
- A new series of 3-hydroxy-2-pyridine aldoxime compounds have been designed, synthesised and tested in vitro, in silico, and ex vivo as reactivators of human acetylcholinesterase (hAChE) and butyrylcholinesterase (hBChE) inhibited by organophosphates (OPs), for example, VX, sarin, cyclosarin, tabun, and paraoxon. (proteopedia.org)
- Organophosphate are absorbed through the skin lungs & GI tract and distributed widely in tissues and are slowly eliminated in hepatic metabolism.The principal effect is inhibition of cholinesterase enzymes, particularly acetylcholinesterase (AChE). (co.ke)
- Poisoning with phosphorus-containing organic chemicals or OP compounds can be managed with antidotes like oximes which are potential reactivators of acetylcholinesterase (AChE). (ac.ir)
- HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs. (nel.edu)
- Oxime HI-6 DMS (dimethanesulfonate) is an asymmetric bis-pyridinium aldoxime and essential acetylcholinesterase (AChE) reactivator. (nel.edu)
- Kuneš M, Květina J, Bureš J, Karasová J, Pavlík M, Tachecí I, Musílek K, Kuca K. HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs. (nel.edu)
Oximes as cholinesterase reactivators3
- Jokanovic M, Stojiljkovic M. Current understanding of the application of pyridinium oximes as cholinesterase reactivators in treatment of organophosphate poisoning. (labome.org)
- Pyridinium oximes as cholinesterase reactivators. (wikipedia.org)
- In Chapter 5, Jokanović and Petrović review pyridinium oximes as cholinesterase reactivators for the treatment of organophosphorus poisoning. (benthamscience.com)
Inhibitors3
- Treatment/antidote of IRReversible cholinesterase inhibitors? (cram.com)
- How does ATROPINE work as a treatment/antidote of IRReversible cholinesterase inhibitors? (cram.com)
- After some time though, some inhibitors can develop a permanent bond with cholinesterase, known as aging, where oximes such as pralidoxime cannot reverse the bond. (gutenberg.org)
Antidotes2
- The military has developed Autoinjector kits (Mark 1 kits) that contain two antidotes, an oxime (an AChE reactivator) and atropine. (medscape.com)
- Known antidotes, which react with the substance and release the substrate (for example, oxime reactivators cholinesterase, similarly, there are antidotes used for poisoning metgemoglobinoobrazovatelami substances). (hindimequotes.com)
Atropine2
- For the immediate treatment of organophosphate poisoning, dry/wet autoinjectors have been developed, containing the broad-spectrum cholinesterase reactivator HI 6 dichloride as a powder and atropine in solution. (mendeley.com)
- atropine and drugs that regenerate the cholinesterase enzyme i.e. (enoeco.com)
Inhibitor2
- Effect on enzymes and other biochemical parameters Fensulfothion, like other organophosphorothionate esters, is a weak cholinesterase inhibitor which, after being converted to the corresponding phosphate ester of fensulfothion is from 500 to 2 000 times more active in inhibiting cholinesterase. (inchem.org)
- Onset of poisoning signs is usually delayed compared with that of many other commonly used organophosphates because of the conversion of chlorpyrifos to the active cholinesterase inhibitor chlorpyrifos-oxon. (org.ua)
AChE2
- This review is centered on the recent developments and structural modification of AChE reactivators against nerve agent toxicity. (eurekaselect.com)
- Among these approaches, determination of inhibition of AChE and BChE functional activity in the blood is still the mainstay for quick initial screening, although determination of relative cholinesterase activity lacks sensitivity and specificity. (aspetjournals.org)
Oxime reactivators1
- We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that contain tertiary amine or imidazole protonatable functional groups. (elsevier.com)
Organophosphates3
- Drugs used to reverse the inactivation of cholinesterase caused by organophosphates or sulfonates. (labome.org)
- Pralidoxime also slows the process of "aging" of phosphorylated cholinesterase to a nonreactivatable form, and detoxifies certain organophosphates by direct chemical reaction. (pharmacycode.com)
- Absorption occurs through all routes Carbamates differ toxicologically from organophoshphates in two ways: 1.They will spontaneously hydrolyse from the cholinesterase enzymatic site within 24 to 48 hours, whereas organophosphates will not 2.They do not effectively penetrate into central nervous system{CNS} and as such CNS toxicity is limited. (pediatriconcall.com)
Aldoxime cholinesterase reactivators1
- Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. (mdpi.com)
Organophosphate5
- Pralidoxime is to reactivate cholinesterase (mainly outside of the central nervous system) which has been inactivated by phosphorylation due to an organophosphate pesticide or related compound. (pharmacycode.com)
- Pralidoxime (2-PAM) is a cholinesterase reactivator and the antidote for organophosphate poisoning. (medscape.com)
- Administer 2-PAM as soon as possible because its effectiveness decreases with prolonged exposure due to the aging of the organophosphate-cholinesterase bond. (medscape.com)
- Potent 3-Hydroxy-2-Pyridine Aldoxime Reactivators of Organophosphate-Inhibited Cholinesterases with Predicted Blood-Brain Barrier Penetration. (proteopedia.org)
- Prevents permanent binding of the organophosphate to cholinesterase. (co.ke)
Pralidoxime chloride2
Anti-cholinesterase activity1
- As with several other compounds of a similar structural nature, cholinesterase activity in females is more sensitive to in vivo anti-cholinesterase activity. (inchem.org)
Irritants and Vesicants1
- Volume 2, Cholinesterase reactivators, psychochemicals, and irritants and vesicants / prepared by the Panel on Cholinesterase Reactivator Chemicals, Panel on Psychochemicals, Panel on Irritants and Vesicants, Committee on Toxicology, Board on Toxicology and Environmental Health Hazards, Commission on Life Sciences, National Research Council. (opal-libraries.org)
Severity3
- It has been reported that the supplemental use of oxime cholinesterase reactivators (such as pralidoxime) reduces the incidence and severity of developmental defects in chick embryos exposed to such known teratogens as parathion, bidrin, carbachol and neostigmine. (nih.gov)
- Usually reaching its cholinesterase reactivator, clear visualization of the authors reporting increases in severity. (puc.edu)
- However, at present, there are men with tpsa between 3 hours for 24 hours follow- reversible increases in severity, usually reaching its cholinesterase reactivator. (puc.edu)
Reactivation5
- In particular, a deeper look has been taken into chemical modifications of the reactivators by incorporation of different structural moieties targeted towards the increased reactivation affinity and improved blood brain barrier (BBB) penetration. (eurekaselect.com)
- Reactivation kinetics of the lead hydroxyimino acetamide reactivator of hAChE, when analyzed in terms of apparent affinity (1/K ox ) and maximum reactivation rate (k 2 ), is superior to the reference uncharged reactivators monoisonitrosoacetone and 2,3-butanedione monoxime and shows potential for further refinement. (elsevier.com)
- The disparate pH dependences for reactivation of ChE and the general base-catalyzed oximolysis of acetylthiocholine reveal that distinct reactivator ionization states are involved in the reactivation of ChE conjugates and in conferring nucleophilic reactivity of the oxime group. (elsevier.com)
- Their reactivation activity was compared with standard reactivators-pralidoxime, obidoxime and HI-6-which are clinically used at present. (mdpi.com)
- Moreover, efficient ex vivo reactivation of phosphylated native cholinesterases by selected oximes enabled significant hydrolysis of VX, sarin, paraoxon, and cyclosarin in whole human blood, which indicates that the oximes have scavenging potential. (proteopedia.org)
Inhibition2
- A few organophosphorus pesticides have produced the so-called "Intermediate Syndrome" and delayed and persistent neuropathy, apparently unrelated to cholinesterase inhibition. (intox.org)
- Following intraperitoneal administration of fensulfothion (0.9 mg/kg) to rats, inhibition of cholinesterase was maximal within one hour. (inchem.org)
Organophosphorus2
- PAM-2), trimedoxime (TMB-4), obidoxime (LüH-6, Toxogonin), HI-6 and HLö-7 which are used as cholinesterase reactivators in the treatment of poisoning with organophosphorus compounds. (labome.org)
- Cholinesterase reactivators and bioscavengers for pre- and post-exposure treatments of organophosphorus poisoning. (ebi.ac.uk)
Conjugates2
- Among the evaluated compounds, two morpholine-3-hydroxypyridine aldoxime conjugates proved to be promising reactivators of OP-inhibited cholinesterases. (proteopedia.org)
- Mechanism of interaction of novel uncharged, centrally active reactivators with OP-hAChE conjugates. (semanticscholar.org)
Insecticides1
- The ATROPEN ® Auto-Injector is indicated for the treatment of poisoning by susceptible organophosphorous nerve agents having cholinesterase activity as well as organophosphorous or carbamate insecticides. (drugs.com)
Structural2
- Rahul Sharma, Bhanushree Gupta, Namrata Singh, J.R. Acharya, Kamil Musilek, Kamil Kuca and Kallol Kumar Ghosh, "Development and Structural Modifications of Cholinesterase Reactivators against Chemical Warfare Agents in Last Decade: A Review", Mini-Reviews in Medicinal Chemistry (2015) 15: 58. (eurekaselect.com)
- The four-helix bundle in cholinesterase dimers: Structural and energetic determinants of stability. (nih.gov)
Reactivates2
- Reactivates cholinesterase after poisoning with anticholinesterase agents. (thefreedictionary.com)
- Reactivates phophorylated acetyl cholinesterase. (co.ke)
Broad-spectrum1
- Due to this fact, it could be designated as a partially broad-spectrum reactivator. (labome.org)
Substrate1
- Time-course of human cholinesterases-catalyzed competing substrate kinetics. (nih.gov)
Intoxication1
- Kuca K, Jun D, Bajgar J. Currently used cholinesterase reactivators against nerve agent intoxication: comparison of their effectivity in vitro. (labome.org)
Activity2
Nerve agent1
- Targeted synthesis of 1-(4-hydroxyiminomethylpyridinium)-3-pyridiniumpropane dibromide--a new nerve agent reactivator. (labome.org)
Infusion1
- 200 to 1000 mg, slow infusion) for its cholinesterase reactivator property. (ciguatera.pf)
Potent1
- A potent oxime for treatment of tabun and cyclosarin-caused intoxications was thus obtained via slight modification of the reactivator structure (compared to trimedoxime and K027). (labome.org)
Compounds1
- Thus, anti-cholinesterase agents poisoning (caused by phosphoorganic compounds) is characterized by cholinergic system enhanced symptoms. (wikiversity.org)
Molecular1
- Effect of a new cholinesterase reactivator, diethixime, on the central nervous system Dopamine receptor subtypes contribution to Homer1a induction: insights into antipsychotic molecular action. (termsreign.ga)
Modification1
- antitrypsin deficiency is most often persists for weeks plus a cholinesterase reactivator, pralidoxime, is an aid to behavior modification. (raseproject.org)
Exposure1
- Pralidoxime (a specific cholinesterase reactivator) should also be started within four hours of exposure [11]. (enoeco.com)
Neutral1
- Equilibration between the neutral and protonated species at physiological pH enables the reactivators to cross the blood-brain barrier and distribute in the CNS aqueous space as dictated by interstitial and cellular pH values. (elsevier.com)
Blood1
- Although a plasma cholinesterase level was not detectable on admission, the patient's red blood cell cholinesterase level was normal when measured after completion of pralidoxime therapy. (cdc.gov)
Hours2
- The use of cholinesterase reactivators depended on administration within 24-48 hours. (childbirthsolutions.com)
- Determine use 20 cialis de bula mg of cholinesterase reactivators depended on administration within 25-48 hours after ingestion. (medimobile.com)