Butyrylcholinesterase: An aspect of cholinesterase (EC 3.1.1.8).Cholinesterase Reactivators: Drugs used to reverse the inactivation of cholinesterase caused by organophosphates or sulfonates. They are an important component of therapy in agricultural, industrial, and military poisonings by organophosphates and sulfonates.Acetylcholinesterase: An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7.Obidoxime Chloride: Cholinesterase reactivator occurring in two interchangeable isomeric forms, syn and anti.Paraoxon: An organophosphate cholinesterase inhibitor that is used as a pesticide.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: Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.CholinesterasesPralidoxime 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.Chemical Warfare Agents: Chemicals that are used to cause the disturbance, disease, or death of humans during WARFARE.Embryonal Carcinoma Stem Cells: The malignant stem cells of TERATOCARCINOMAS, which resemble pluripotent stem cells of the BLASTOCYST INNER CELL MASS. The EC cells can be grown in vitro, and experimentally induced to differentiate. They are used as a model system for studying early embryonic cell differentiation.Carcinoma, Embryonal: A highly malignant, primitive form of carcinoma, probably of germinal cell or teratomatous derivation, usually arising in a gonad and rarely in other sites. It is rare in the female ovary, but in the male it accounts for 20% of all testicular tumors. (From Dorland, 27th ed & Holland et al., Cancer Medicine, 3d ed, p1595)Cell Differentiation: Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.Carboxylic Ester Hydrolases: Enzymes which catalyze the hydrolysis of carboxylic acid esters with the formation of an alcohol and a carboxylic acid anion.Teratoma: A true neoplasm composed of a number of different types of tissue, none of which is native to the area in which it occurs. It is composed of tissues that are derived from three germinal layers, the endoderm, mesoderm, and ectoderm. They are classified histologically as mature (benign) or immature (malignant). (From DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1642)Tritolyl Phosphates: A mixture of isomeric tritolyl phosphates. Used in the sterilization of certain surgical instruments and in many industrial processes.Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).Sea-Blue Histiocyte Syndrome: A congenital disease caused by an inborn error involving APOLIPOPROTEINS E leading to abnormal LIPID METABOLISM and the accumulation of GLYCOSPHINGOLIPIDS, particularly SPHINGOMYELINS in the HISTIOCYTES. This disorder is characterized by SPLENOMEGALY and the sea-blue histiocytes in the spleen and bone marrow after May Grunwald staining.Organophosphorus Compounds: Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.Mineral Waters: Water naturally or artificially infused with mineral salts or gases.Thiocholine: A mercaptocholine used as a reagent for the determination of CHOLINESTERASES. It also serves as a highly selective nerve stain.Dithionitrobenzoic Acid: A standard reagent for the determination of reactive sulfhydryl groups by absorbance measurements. It is used primarily for the determination of sulfhydryl and disulfide groups in proteins. The color produced is due to the formation of a thio anion, 3-carboxyl-4-nitrothiophenolate.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Sulfhydryl Compounds: Compounds containing the -SH radical.Acetylthiocholine: An agent used as a substrate in assays for cholinesterases, especially to discriminate among enzyme types.Thyroid Neoplasms: Tumors or cancer of the THYROID GLAND.Cyclohexylamines: A family of alicyclic hydrocarbons containing an amine group with the general formula R-C6H10NH2.Antibodies, Bispecific: Antibodies, often monoclonal, in which the two antigen-binding sites are specific for separate ANTIGENIC DETERMINANTS. They are artificial antibodies produced by chemical crosslinking, fusion of HYBRIDOMA cells, or by molecular genetic techniques. They function as the main mediators of targeted cellular cytotoxicity and have been shown to be efficient in the targeting of drugs, toxins, radiolabeled haptens, and effector cells to diseased tissue, primarily tumors.Tetracyclines: Closely congeneric derivatives of the polycyclic naphthacenecarboxamide. (Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1117)Carcinoma: A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm but is often wrongly used as a synonym for "cancer." (From Dorland, 27th ed)Trehalase: An enzyme that catalyzes the conversion of alpha,alpha-trehalose and water to D-glucose. EC 3.2.1.28.Work of Breathing: RESPIRATORY MUSCLE contraction during INHALATION. The work is accomplished in three phases: LUNG COMPLIANCE work, that required to expand the LUNGS against its elastic forces; tissue resistance work, that required to overcome the viscosity of the lung and chest wall structures; and AIRWAY RESISTANCE work, that required to overcome airway resistance during the movement of air into the lungs. Work of breathing does not refer to expiration, which is entirely a passive process caused by elastic recoil of the lung and chest cage. (Guyton, Textbook of Medical Physiology, 8th ed, p406)Drug Utilization: The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.Adenocarcinoma, Follicular: An adenocarcinoma of the thyroid gland, in which the cells are arranged in the form of follicles. (From Dorland, 27th ed)TrehaloseEncyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Antipruritics: Agents, usually topical, that relieve itching (pruritus).Administration, Topical: The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.Dermatology: A medical specialty concerned with the skin, its structure, functions, diseases, and treatment.Pruritus: An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.Dexamethasone: An anti-inflammatory 9-fluoro-glucocorticoid.Databases, Pharmaceutical: Databases devoted to knowledge about PHARMACEUTICAL PRODUCTS.Receptors, Glucocorticoid: Cytoplasmic proteins that specifically bind glucocorticoids and mediate their cellular effects. The glucocorticoid receptor-glucocorticoid complex acts in the nucleus to induce transcription of DNA. Glucocorticoids were named for their actions on blood glucose concentration, but they have equally important effects on protein and fat metabolism. Cortisol is the most important example.Ophthalmic Solutions: Sterile solutions that are intended for instillation into the eye. It does not include solutions for cleaning eyeglasses or CONTACT LENS SOLUTIONS.Pharmacological Processes: The metabolism of drugs and their mechanisms of action.Carotid Artery Diseases: Pathological conditions involving the CAROTID ARTERIES, including the common, internal, and external carotid arteries. ATHEROSCLEROSIS and TRAUMA are relatively frequent causes of carotid artery pathology.Aryldialkylphosphatase: An enzyme which catalyzes the hydrolysis of an aryl-dialkyl phosphate to form dialkyl phosphate and an aryl alcohol. It can hydrolyze a broad spectrum of organophosphate substrates and a number of aromatic carboxylic acid esters. It may also mediate an enzymatic protection of LOW DENSITY LIPOPROTEINS against oxidative modification and the consequent series of events leading to ATHEROMA formation. The enzyme was previously regarded to be identical with Arylesterase (EC 3.1.1.2).Carotid Arteries: Either of the two principal arteries on both sides of the neck that supply blood to the head and neck; each divides into two branches, the internal carotid artery and the external carotid artery.Carotid Stenosis: Narrowing or stricture of any part of the CAROTID ARTERIES, most often due to atherosclerotic plaque formation. Ulcerations may form in atherosclerotic plaques and induce THROMBUS formation. Platelet or cholesterol emboli may arise from stenotic carotid lesions and induce a TRANSIENT ISCHEMIC ATTACK; CEREBROVASCULAR ACCIDENT; or temporary blindness (AMAUROSIS FUGAX). (From Adams et al., Principles of Neurology, 6th ed, pp 822-3)Arteriosclerosis: Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.Carotid Artery, Internal: Branch of the common carotid artery which supplies the anterior part of the brain, the eye and its appendages, the forehead and nose.EsterasesCarotid Artery, Common: The two principal arteries supplying the structures of the head and neck. They ascend in the neck, one on each side, and at the level of the upper border of the thyroid cartilage, each divides into two branches, the external (CAROTID ARTERY, EXTERNAL) and internal (CAROTID ARTERY, INTERNAL) carotid arteries.Atherosclerosis: A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.Endarterectomy, Carotid: The excision of the thickened, atheromatous tunica intima of a carotid artery.

Inhibition of esterolysis of enalapril by paraoxon increases the urinary clearance in isolated perfused rat kidney. (1/149)

The effect of competing elimination pathways on the metabolic and excretory clearance estimates was examined with tracer concentrations of [(3)H]enalapril, which was both metabolized and excreted by the rat kidney. Perturbation was achieved with use of the carboxylesterase inhibitor paraoxon, which inhibited [(3)H]enalapril metabolism to [(3)H]enalaprilat in rat renal S9 fraction. At 0.1, 0.5, 1, and 10 microM paraoxon, esterolysis of enalapril was inhibited by 76 +/- 7, 93 +/- 5, 96 +/- 5, and 93 +/- 6%, respectively. The lowest concentration (0.1 microM) of paraoxon was chosen for single-pass isolated perfused kidney (IPK) studies because viability was least compromised, and the sodium and glucose reabsorptive functions of the IPK remained constant. After an equilibration period (15-20 min at constant pressure, 90-100 mm Hg), perfusion of the rat kidney with [(3)H]enalapril was carried out under constant flow (8 ml/min) for 30 min in the absence and presence of paraoxon (0.1 microM). The metabolic (from 1.83 +/- 0.52 to 1.48 +/- 0.47 ml/min/g) and total renal (from 1.87 +/- 0.46 to 1. 57 +/- 0.41 ml/min/g) clearances of [(3)H]enalapril in the IPKs were decreased significantly (p <.05) in the presence of paraoxon when compared with controls. Concomitantly, the urinary clearance (from 0. 04 +/- 0.07 to 0.09 +/- 0.09 ml/min/g) and the fractional excretion (from 0.23 +/- 0.18 to 0.52 +/- 0.25) of [(3)H]enalapril doubled (p <.05). The study illustrates that a reduction in cellular metabolism of the kidney brings forth a rise in the estimate of clearance of its complimentary pathway, estimate of the excretory (urinary) clearance.  (+info)

Calcium channels involved in the inhibition of acetylcholine release by presynaptic muscarinic receptors in rat striatum. (2/149)

1. The mechanism of the inhibitory action of presynaptic muscarinic receptors on the release of acetylcholine from striatal cholinergic neurons is not known. We investigated how the electrically stimulated release of [3H]-acetylcholine from superfused rat striatal slices and its inhibition by carbachol are affected by specific inhibitors of voltage-operated calcium channels of the L-type (nifedipine), N-type (omega-conotoxin GVIA) and P/Q-type (omega-agatoxin IVA). 2. The evoked release of [3H]-acetylcholine was not diminished by nifedipine but was lowered by omega-conotoxin GVIA and by omega-agatoxin IVA, indicating that both the N- and the P/Q-type (but not the L-type) channels are involved in the release. The N-type channels were responsible for approximately two thirds of the release. The release was >97% blocked when both omega-toxins acted together. 3. The inhibition of [3H]-acetylcholine release by carbachol was not substantially affected by the blockade of the L- or P/Q-type channels. It was diminished but not eliminated by the blockade of the N-type channels. 4. In experiments on slices in which cholinesterases had been inhibited by paraoxon, inhibition of [3H]-acetylcholine release by endogenous acetylcholine accumulating in the tissue could be demonstrated by the enhancement of the release after the addition of atropine. The inhibition was higher in slices with functional N-type than with functional P/Q-type channels. 5. We conclude that both the N- and the P/Q-type calcium channels contribute to the stimulation-evoked release of acetylcholine in rat striatum, that the quantitative contribution of the N-type channels is higher, and that the inhibitory muscarinic receptors are more closely coupled with the N-type than with the P/Q-type calcium channels.  (+info)

Stability of cytotoxic luteinizing hormone-releasing hormone conjugate (AN-152) containing doxorubicin 14-O-hemiglutarate in mouse and human serum in vitro: implications for the design of preclinical studies. (3/149)

Recently, we developed a series of cytotoxic peptide conjugates containing 14-O-glutaryl esters of doxorubicin (DOX) or 2-pyrrolino-DOX (AN-201). Serum carboxylesterase enzymes (CE) can partially hydrolyze these conjugates in the circulation, releasing the cytotoxic radical, before the targeting is complete. CE activity in serum of nude mice is about 10 times higher than in human serum. Thus, we found that the t(1/2) of AN-152, an analog of luteinizing hormone-releasing hormone (LH-RH) containing DOX, at 0.3 mg/ml is 19. 49 +/- 0.74 min in mouse serum and 126.06 +/- 3.03 min in human serum in vitro. The addition of a CE inhibitor, diisopropyl fluorophosphate (DFP), to mouse serum in vitro significantly (P < 0. 01) prolongs the t(1/2) of AN-152 to 69.63 +/- 4.44 min. When DFP is used in vivo, 400 nmol/kg cytotoxic somatostatin analog AN-238 containing AN-201 is well tolerated by mice, whereas all animals die after the same dose without DFP. In contrast, DFP has no effect on the tolerance of AN-201. A better tolerance to AN-238 after DFP treatment is due to the selective uptake of AN-238 by somatostatin receptor-positive tissues. Our results demonstrate that the suppression of the CE activity in nude mice greatly decreases the toxicity of cytotoxic hybrids containing 2-pyrrolino-DOX 14-O-hemiglutarate and brings this animal model closer to the conditions that exist in humans. The use of DFP together with these peptide conjugates in nude mice permits a better understanding of their mechanism of action and improves the clinical predictability of the oncological and toxicological results.  (+info)

Placental transfer and pharmacokinetics of a single dermal dose of [14C]methyl parathion in rats. (4/149)

The pharmacokinetics and placental transfer of a single dermal 10.0 mg (10microCi)/kg dose of uniformly phenyl-labeled [14C] methyl parathion (0,0-dimethyl 0-4-nitrophenyl phosphorothioate) were investigated in pregnant Sprague-Dawley rats at 14-18 days of gestation. Three rats were killed at each time interval: 1, 2, 4, 12, 24, 48, 72, and 96 h after dosing. Radioactivity disappeared biexponentially from the administration sites, which retained 50% and 3% of the dose after 1 h and 96 h, respectively. Most of the absorbed radioactivity was excreted in the urine (91%). Only 3% of the 14C was recovered in the feces. One h after the administration, radioactivity was detected in all tissues, including fetal tissue. The peak maternal plasma concentration of radioactivity (ng methyl parathion equivalent/ml) was 1005 at 2 h, compared to 318 ng for fetal plasma at 12 h. The maximum concentrations of radioactivity (ng methyl parathion equivalent/g), detected in most tissues within 12 h of dosing, were, in descending order: adipose tissue (67,532), kidney (1,571), spleen (1,256), spinal cord (1,004), heart (729), liver (706), brain (546), placenta (389), and fetus (256). The metabolism studies showed that methyl parathion, detected by HPLC, was the major compound identified in plasma and tissues. The maximum concentration detected was in plasma, at 513 ng/ml, and in the following tissues (ng/g fresh tissue): kidney (819), fetus (668), placenta (394), liver (375), and brain (282). The metabolite methyl paraoxon was detected in maternal brain and liver at maximum concentrations (ng/g fresh tissue) of 135 and 64 after 12 h and 4 h respectively, while p-nitrophenol was only detected in liver at a maximum concentration of 21 ng/g 72 h after dosing. Pharmacokinetic studies showed that methyl parathion disappeared monoexponentially from plasma and tissues. The half-life of elimination of methyl parathion from plasma was 11 h corresponding to a constant rate value of 0.06 h(-1). The results indicate that skin and placenta are poor barriers against methyl parathion permeability, resulting in a rapid and extensive dermal absorption of this insecticide and extensive placental transfer. This is indicated by the relative residence (R(R)) of methyl parathion in the plasma, which was largest in the placenta followed by the fetus. This study suggests that pregnant women and fetuses may be at risk of cholinergic toxicity following dermal exposure to methyl parathion.  (+info)

Critical role of micelles in pancreatic lipase activation revealed by small angle neutron scattering. (5/149)

In the duodenum, pancreatic lipase (PL) develops its activity on triglycerides by binding to the bile-emulsified oil droplets in the presence of its protein cofactor pancreatic colipase (PC). The neutron crystal structure of a PC-PL-micelle complex (Hermoso, J., Pignol, D., Penel, S., Roth, M., Chapus, C., and Fontecilla-Camps, J. C. (1997) EMBO J. 16, 5531-5536) has suggested that the stabilization of the enzyme in its active conformation and its adsorption to the emulsified oil droplets are mediated by a preformed lipase-colipase-micelle complex. Here, we correlate the ability of different amphypathic compounds to activate PL, with their association with PC-PL in solution. The method of small angle neutron scattering with D(2)O/H(2)O contrast variation was used to characterize a solution containing PC-PL complex and taurodeoxycholate micelles. The resulting radius of gyration (56 A) and the match point of the solution indicate the formation of a ternary complex that is similar to the one observed in the neutron crystal structure. In addition, we show that either bile salts, lysophospholipids, or nonionic detergents that form micelles with radii of gyration ranging from 13 to 26 A are able to bind to the PC-PL complex, whereas smaller micelles or nonmicellar compounds are not. This further supports the notion of a micelle size-dependent affinity process for lipase activation in vivo.  (+info)

Nitric oxide is involved in acetylcholinesterase inhibitor-induced myopathy in rats. (6/149)

Excess activation of muscle nicotinic acetylcholine receptors due to genetic mutations, as seen in slow channel congenital myasthenic syndrome, or acetylcholinesterase (AChE) inhibition results in muscle cell degeneration. Our recent work showed that nitric oxide synthase (NOS) inhibitors prevent nicotine-induced muscle cell death in culture. In the present study, we examined the effects of NOS inhibition on nicotinic receptor-mediated myopathy in vivo. Rats injected with the AChE inhibitor paraoxon demonstrate a 90-fold increase in the number of dying muscle cells compared with control as evidenced histologically by centralized nuclei and the presence of degenerating profiles. Coadministration of the nonspecific NOS inhibitor nitro-L-arginine methyl ester or the neuronal NOS-specific inhibitor 7-nitroindazole dramatically reduced the presence of such degenerating profiles to approximately 20% of that seen with paraoxon alone. These results show that inhibition of NOS, as well as neuronal NOS, significantly reduces AChE inhibitor-induced muscle cell degeneration, suggesting that increased nitric oxide production mediates such myopathy.  (+info)

Interactions of the organophosphates paraoxon and methyl paraoxon with mouse brain acetylcholinesterase. (7/149)

The mechanism of acute toxicity of the organophosphorus insecticides has been known for many years to be inhibition of the critical enzyme acetylcholinesterase (EC 3.1.1.7), with the resulting excess acetylcholine accumulation leading to symptoms of cholinergic excess. The bimolecular inhibition rate constant k(i) has been used for decades to describe the inhibitory capacity of organophosphates toward acetylcholinesterase. In the current study, a new approach based on continuous systems modeling was used to determine the appk(i)s of paraoxon and methyl paraoxon towards mouse brain acetylcholinesterase over a wide range of oxon concentrations. These studies revealed that the bimolecular inhibition rate constants for paraoxon and methyl paraoxon appeared to change as a function of oxon concentrations. For example, the appk(i) found with a paraoxon concentration of 1000 nM was 0.16 nM-1h-1, whereas that for 0.1 nM paraoxon was 1.60 nM-1h-1, indicating that the efficiency of phosphorylation appeared to decrease as the paraoxon concentration increased. These data suggested that the current understanding of how these organophosphates interact with acetylcholinesterase is incomplete. Modeling studies using several different kinetic schemes, as well as studies using recombinant monomeric mouse brain acetylcholinesterase, suggested the existence of a second binding site in addition to the active site of the enzyme, to which paraoxon and methyl paraoxon bound, probably in a reversibly manner. Occupation of this site likely rendered more difficult the subsequent phosphorylation of the active site by other oxon molecules, probably by steric hindrance or allosteric modification of the active site. It cannot be ascertained from the current study whether the putative second binding site is identical to or shares common elements with the well-characterized propidium-specific peripheral binding site of acetylcholinesterase.  (+info)

Paraoxonase (PON1) phenotype is a better predictor of vascular disease than is PON1(192) or PON1(55) genotype. (8/149)

The paraoxonase (PON1) PON1-Q192R and PON1-L55M polymorphisms have been inconsistently associated with vascular disease. Plasma PON1 activity phenotypes vary markedly within genotypes and were, therefore, expected to add to the informativeness of genotype for predicting vascular disease. The case-control sample included 212 age- and race-matched men (mean age 66.4 years). The 106 carotid artery disease (CAAD) cases had >80% carotid stenosis, and the 106 controls had <15%. Two PON1 substrate hydrolysis rates (paraoxon [POase] and diazoxon [DZOase]) were significantly lower in cases than in controls and were significant predictors of CAAD by use of logistic regression (POase, P=0.005; DZOase, P=0.019). DZOase predicted vascular disease independently of lipoprotein profile, high density lipoprotein subfractions, apolipoprotein A-I, and smoking. PON1-192 and PON1-55 genotypes or haplotypes did not predict case-control status unless the activity phenotype was also included as a predictor by use of logistic regression. When phenotype was included as a predictor, PON1-192 and PON1-55 genotypes or combined haplotypes were significant predictors (P<0.05). In conclusion, examining PON1-192 and/or PON1-55 genotypes alone may mistakenly lead to the conclusion that there is no role of PON1 in CAAD. These results support the benefit of a "level crossing" approach that includes intervening phenotypes in the study of complexly inherited disease.  (+info)

*Paraoxon

... has been used by scientists to study acute and chronic effects of organophosphate intoxication. It is easily absorbed ... Paraoxon is one of the most potent acetylcholinesterase-inhibiting insecticides available, around 70% as potent as the nerve ... Paraoxon is a parasympathomimetic which acts as an acetylcholinesterase inhibitor. It is an organophosphate oxon, and the ... NTI Country Overviews:South Africa:Chemical Capabilities:Paraoxon. ...

*Oxon (chemical)

Paraoxon Chlorpyrifos oxon. ...

*Parathion

Absorbed parathion is rapidly metabolized to paraoxon, as described in Insecticidal activity. Paraoxon exposure can result in ... After an insect (or a human) ingests parathion, an oxidase replaces the double bonded sulfur with oxygen to give paraoxon. ( ...

*Francesco De Lorenzo

Screening of 24 pesticides by the Salmonella/microsome assay: mutagenicity of Benazolin, Metoxuron and Paraoxon. X Annual ...

*Ecogenetics

1] Pharmacogenetics Pesticide Organophosphate Parathion Paraoxon Paraoxonase Nerve gas Soman Sarin Cummings, Michael R. Human ...

*Paraoxonase

The name paraoxonase was given because of its ability to hydrolyze paraoxon, a toxic metabolite that comes from pesticide ...

*Aryldialkylphosphatase

It does not seem to have a natural occurring substrate and may thus have optimally evolved for utilizing paraoxon and other ... The turnover rate (kcat) of phosphotriesterase is nearly 104 s−1 for the hydrolysis of paraoxon, and the products are p- ... The enzyme has a very broad substrate specificity, and is very efficient in catalyzing the reaction: PTE hydrolyzes paraoxon at ...

*Phenols

Aryldialkylphosphatase (also known as organophosphorus hydrolase, phosphotriesterase, and paraoxon hydrolase) uses an aryl ...

*Aromatic alcohol

Aryldialkylphosphatase (also known as organophosphorus hydrolase, phosphotriesterase, and paraoxon hydrolase) uses an aryl ...

*PON1

Some substrates e.g. paraoxon are hydrolysed faster by the R- isoform while others such as diazoxon and lipid-peroxides are ...

*ATC code S01

S01EB05 Physostigmine S01EB06 Neostigmine S01EB07 Fluostigmine S01EB08 Aceclidine S01EB09 Acetylcholine S01EB10 Paraoxon ...
Diethyl p-nitrophenyl phosphate (paraoxon) is the active toxic metabolite of parathion. Some evidences indicate that OPs affect the GABA system via noncholinergic mechanisms. The purpose of this study was to investigate the effects of paraoxon on K+-evoked [3H]-GABA release from cerebellar synaptosomes. Adult male rats (200 ± 30 g; 3-4 months old) were sacrificed by decapitation and the cerebellum was removed immediately and homogenized. Homogenate was centrifuged twice at 1000 × g for 5 min (all in 0-4 ?C). Synaptosomes were incubated with [3H]-GABA (S.A 99 Ci/mmol, 0.1 µm). Then, aliquots of the synaptosomal suspension were layered on microporous filters at the bottom of superfusion chambers (14900 Superfusion System, Raiteri,s Method, UGO BASILE, Italy). Following 34 minutes of superfusion (time required to equilibrate the system, t = 0), fractions were collected every minute and the radioactivity in the different samples was quantified by liquid-scintillation counting. At t = 8 (s1) and t = 28
A cholinesterase based biosensor was constructed in order to assess the effects of ionizing radiation on exposed AChE. Although the primary objective of the experiment was to investigate the effect of ionizing radiation on the activity of the biosensor, no changes in cholinesterase activity were observed. Current provided by oxidation of thiocholine previously created from acetylthiocholine by enzyme catalyzed reaction was in a range 395-455 nA. No significant influence of radiation on AChE activity was found, despite the current variation. However, a surprising phenomenon was observed when a model organophosphate paraoxon was assayed. Irradiated biosensors seem to be more susceptible to the inhibitory effects of paraoxon. Control biosensors provided a 94 ± 5 nA current after exposure to 1 ppm paraoxon. The biosensors irradiated by a 5 kGy radiation dose and exposed to paraoxon provided a current of 49 ± 6 nA. Irradiation by doses ranging from 5 mGy to 100 kGy were investigated and the mentioned
The bacterial phosphotriesterases catalyze hydrolysis of the pesticide paraoxon with very fast turnover rates and are thought to be near to their evolutionary limit for this activity. To test whether the naturally evolved turnover rate could be improved through the incorporation of unnatural amino acids and to probe the role of peripheral active site residues in nonchemical steps of the catalytic cycle (substrate binding and product release), we replaced the naturally occurring tyrosine amino acid at position 309 with unnatural L-(7-hydroxycoumarin-4-yl)ethylglycine (Hco) and L-(7-methylcoumarin-4-yl)ethylglycine amino acids, as well as leucine, phenylalanine, and tryptophan. Kinetic analysis suggests that the 7-hydroxyl group of Hco, particularly in its deprotonated state, contributes to an increase in the rate-limiting product release step of substrate turnover as a result of its electrostatic repulsion of the negatively charged 4-nitrophenolate product of paraoxon hydrolysis. The 8-11-fold ...
Has an unusual substrate specificity for synthetic organophosphate triesters and phosphorofluoridates. All of the phosphate triesters found to be substrates are synthetic compounds. The identity of any naturally occurring substrate for the enzyme is unknown. Has no detectable activity with phosphate monoesters or diesters and no activity as an esterase or protease. It catalyzes the hydrolysis of the insecticide paraoxon at a rate approaching the diffusion limit and thus appears to be optimally evolved for utilizing this synthetic substrate ...
Ondracek K, Bandouchova H, Hilscherova K, Kovacova V, Linhart P, Miksikova M, Mlcakova V, Osickova J, Pohanka M, Skochova H, Pikula J. Mixture toxicity of microcystin-LR, paraoxon and bromadiolone in Xenopus laevis embryos. Neuro Endocrinol Lett. 2015 Jan; 36(Suppl 1): 114-119 ...
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex assemblies. As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
Authors: MIROSLAV POHANKA, JANA ZDAROVA KARASOVA, KAMIL KUCA, JIRI PIKULA Abstract: Multichannel spectrophotometry was performed to assay for paraoxon in spiked beverages. A 96-well microplate was used for this purpose. The measuring protocol was based on inhibition of the enzyme acetylcholinesterase by paraoxon that resulted in decreased or no reaction of the enzyme product thiocholine with Ellmans reagent (5,5-dithiobis [2-nitrobenzoic acid]). The above assay was practically tested using spiked drinking water, mineral water, and coffee. Analytical parameters such as the limit of detection, time, and sample size consumption were adequate. The limit of detection for beverages ranged from 32 to 48 ppb corresponding to 0.32-0.48 ng of paraoxon in absolute values. The described assay seems to be convenient in terms of practical use. Keywords: Acetylcholinesterase, cholinesterase, biosensing, pesticides, assay, Ellman. Full Text: PDF ...
The catalytic bioscavenger phosphotriesterase (PTE) is experimentally an effective antidote for organophosphate poisoning. We are interested in the molecular engineering of this enzyme to confer additional functionality, such as improved in vivo longevity. To this aim, we developed PTE cysteine mutants with free sulfhydryls to allow macromolecular attachments to the protein. A library of PTE cysteine mutants were assessed for efficiency in hydrolysing the toxic pesticide metabolite paraoxon, and screened for attachment with a sulfhydryl-reactive small molecule, fluorescein 5-maleimide (F5M), to examine cysteine availability. We established that the newly incorporated cysteines were readily available for labelling, with R90C, E116C and S291C displaying the highest affinity for binding with F5M. Next, we screened for efficiency in attaching a large macromolecule, a 30 000 Da polyethylene glycol (PEG) molecule. Using a solid-phase PEGylation strategy, we found the E116C mutant to be the best single-mutant
The transport of neurotoxic esterase (NTE) was studied in the sciatic nerve of the White-leghorn-hen. Measurements were taken of the rate of accumulation of activity at either one or two ligations. NTE appeared to be transported down the sciatic nerve at a rate of 300 millimeters/day. Acetylcholinesterase was transported at a rate of about 500 millimeters/day. The movement of NTE between transport
Prophylactic protection by intraperitoneally administered l-methyl-2-formylpyridinium iodide oxime (2-PAM) against tetraethylpyrophosphate, paraoxon and diisopropyl phosphorofluoridate intoxication in mice was markedly enhanced by intracerebral administration of this antagonist into the central nervous system.. Potency ratios and LD50 values of these alkylphosphates were compared in groups of mice premedicated with 2-PAM and/or atropine. The 2-PAM was administered by the intraperitoneal, intracerebral, and combined intracerebral-intraperitoneal route.. These results indicated that the intracerebral administration of 2-PAM alone had little or no effect in antagonizing these alkylphosphates. Although some protection was afforded by 2-PAM intraperitoneally, its effects were markedly enhanced by combined administration of 2-PAM by the intracerebral-intraperitoneal routes. These effects were even more striking when tested in combination with atropine sulfate. The most effective protection against ...
This terminal progress report reviews and summarizes the earlier work. The oxygen analogs of the organophosphothionate pesticides are readily formed in the field, are relatively persistent, and are often the principal toxic constituents of the weathered residues. The conversion of ethyl-parathion to (56382) paraoxon (311455) is related to air pollution levels, and for some pesticides the foliar de
doi: 10.1016/j.abb.2005.08.012, 10.1002/0471264180.or025.02 oph: A organo-phosphate (P-O) hydroxyl bound to a ketone or aldehyde. Synthetic intermediate and precursor to organo-phosphate agents known as AChE inhibitors. Reaction is catalyzed by the Organo-Phosphate Hydrolase enzyme, thus a (Mg)ATP-dependent ligase. See related DOIs above. dfp (Isoflurophate): http://www.drugbank.ca/drugs/DB00677, Wikipedia EC 3.1.8.2 (DFPase) http://www.genome.jp/dbget-bin/www_bget?ec:3.1.8.2 EC 3.1.8.1 (Parathion hydrolase) http://www.uniprot.org/uniprot/P0A433, http://www.drugbank.ca/drugs/DB02138 HMDB keywords: functionalized diphosphine, chim trills, DFP, Paraoxon Reaction type: oxidative desulfuration (BioCyc) Related: 3-phosphoinositide-dependent protein kinase 1, Serine/threonine-protein phosphatase 2A 55 kDa regulatory subunit B beta isoform Regulation of 3-Phosphoinositide-dependent Protein Kinase-1 (PDK1) by Src Involves Tyrosine Phosphorylation of PDK1 and Src Homology 2 Domain Binding ...
1DPM: Three-dimensional structure of the zinc-containing phosphotriesterase with the bound substrate analog diethyl 4-methylbenzylphosphonate.
The presence of a cathepsin B-like enzyme in rabbit ear cartilage was established by the use of the synthetic substrates benzoyl-l-arginine amide and benzoyl-dl-arginine 2-naphthylamide. This was facilitated by using a technique that permits the incubation of a fixed weight of thin (18μ) cartilage sections with an appropriate exogenous substrate. The enzymic properties of cathepsin B in cartilage have been compared with an endogenous enzyme that liberates chondromucopeptide by degrading the cartilage matrix autocatalytically at pH5. Besides being maximally active at pH4·7, these cartilage enzymes are enhanced in activity by cysteine and inhibited by arginine analogues, iodoacetamide, chloroquine and mercuric chloride. They are not inhibited by EDTA, di-isopropyl phosphorofluoridate and diethyl p-nitrophenyl phosphate. When inhibiting the release of chondromucopeptide from cartilage at pH5, the arginine-containing synthetic substrates are hydrolysed simultaneously. These enzymes also share the ...
1. The distribution of individual phospholipids was determined in hen brain and compared with that in sciatic nerve obtained in a previous investigation. Sciatic nerve is more enriched in the myelinic phospholipids ethanolamine plasmalogen, phosphatidylserine and sphingomyelin, but it contains relatively less triphosphoinositide, and much less diphosphoinositide, than the brain. 2. The course of incorporation of intraperitoneally injected 32P into the acid-soluble phosphorus, phosphoinositides and total phospholipids of hen brain and sciatic nerve was followed. Although the maximum specific radioactivity in sciatic nerve of acid-soluble phosphorus is 4·5 times, and that of triphosphoinositide six times, that in the brain, the relative rate of triphosphoinositide phosphorus synthesis per gram of brain is three times that in sciatic nerve. 3. Administration of the demyelinating agent tri-o-cresyl phosphate to hens has no significant effect on the amounts or the rate of 32P incorporation into the ...
Historically, only few chemicals have been identified as neurodevelopmental toxicants, however, concern remains, and has recently increased, based upon the association between chemical exposures and increased developmental disorders. Diminution in motor speed and latency has been reported in preschool children from agricultural communities. Organophosphorus compounds (OPs) are pesticides due to their acute insecticidal effects mediated by the inhibition of acetylcholinesterase, although other esterases as neuropathy target esterase (NTE) can also be inhibited. Other neurological and neurodevelopmental toxic effects with unknown targets have been reported after chronic exposure to OPs in vivo. We studied the initial stages of retinoic acid acid-triggered differentiation of pluripotent cells towards neural progenitors derived from human embryonal carcinoma stem cells to determine if neuropathic OP, mipafox, and non-neuropathic OP, paraoxon, are able to alter differentiation of neural precursor cells in
Esterases represent an ancient family of enzymes, found across all kingdoms, which have diverged and occupied a wide range of functional niches. Because of their biochemical diversity and electrophoretic variability, esterases are widely used as genetic markers in gel electrophoresis assays, yet they remain ill-defined. The aim of this study is to characterise esterases from plants with roles in both normal cellular metabolism as well as in xenobiotic metabolism. A survey of esterase activities in four species of crop plants (Triticum aestivum, Zea mays, Glycine max and Oryza sativa) and Arabidopsis thaliana has shown that most of the esterases were typical carboxylesterases containing a catalytically active serine residue. Esterases varied considerably between plants according to their electrophoretic mobility and their substrate specificity. However, their sensitivities to inhibitors were broadly similar with serine hydrolase inhibitors, such as paraoxon, abolishing most esterolytic activify. ...
Mono- and Stereopictres of 5.0 Angstrom coordination sphere of Arsenic atom in PDB 2o4m: Structure of Phosphotriesterase Mutant I106G/F132G/H257Y
Article Characterization of phosphorus sources in rural watersheds. Received for publication February 21, 2008. Correct identification of P sources in rural watersheds is critical for the development of cost-effective measures to combat agriculturall...
Two major isoforms of human carboxylesterases (CEs) are found in metabolically active tissues, CES1 and CES2. These hydrolytic enzymes are involved in xenobiotic and endobiotic metabolism. CES1 is abundantly expressed in human liver and monocytes/mac
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Hydrolyzes the toxic metabolites of a variety of organophosphorus insecticides. Capable of hydrolyzing a broad spectrum of organophosphate substrates and lactones, and a number of aromatic carboxylic acid esters. Mediates an enzymatic protection of low density lipoproteins against oxidative modification.
Human Carboxylesterase 1 (hCES1) is the key liver microsomal enzyme responsible for detoxification and metabolism of a variety of clinical drugs. To analyse the role of the single N-linked glycan on the structure and activity of the enzyme, authentically glycosylated and aglycosylated hCES1, generated by mutating asparagine 79 to glutamine, were produced in human embryonic kidney cells. Purified enzymes were shown to be predominantly trimeric in solution by analytical ultracentrifugation. The purified aglycosylated enzyme was found to be more active than glycosylated hCES1 and analysis of enzyme kinetics revealed that both enzymes exhibit positive cooperativity. Crystal structures of hCES1 a catalytically inactive mutant (S221A) and the aglycosylated enzyme were determined in the absence of any ligand or substrate to high resolutions (1.86 Å, 1.48 Å and 2.01 Å, respectively). Superposition of all three structures showed only minor conformational differences with a root mean square deviations ...
Serum paraoxonase/arylesterase 1 (PON1) also known as A esterase , homocysteine thiolactonase or serum aryldialkylphosphatase 1 is an enzyme that in humans is encoded by the PON1 gene. Paraoxonase 1 has esterase and more specifically paraoxonase activity. Serum PON1 is found in all mammalian species studied so far but is not present in the serum of birds, fish and reptiles or in insects. PON1 is the first discovered member of a multigene family also containing PON2 and PON3, the genes for which are located adjacent to each other on chromosome 7. Human PON1 is a glycoprotein composed of 354 amino acids and has a molecular weight of 43000 Daltons which associates with high-density lipoprotein (HDL, "good cholesterol") in the circulation. Serum PON1 is secreted mainly by the liver although local synthesis occurs in several tissues and PON1 protein is found in almost all tissues. X-ray crystallography has revealed the structure of PON1 to be a 6 bladed propeller with a unique lid structure covering ...
Sigma-Aldrich offers abstracts and full-text articles by [M Aviram, M Rosenblat, S Billecke, J Erogul, R Sorenson, C L Bisgaier, R S Newton, B La Du].
The title compd. (also known as kresoxim-methyl), $C_1_8H_1_9NO_4$, is an active agrochem. exhibiting fungicidal activity. Crystallog. data are given. The dihedral angle between the two rings is 65.9(1)°. The crystal structure is stabilized by weak but highly directional $C-H\cdot\cdot\cdotO$ and $C-H\cdot\cdot\cdot\pi$ intermolecular interactions.. ...
Human serum paraoxonase/arylesterase 1 (PON1) standard, for use in running standard curves in AlphaLISA detection and quantitation assays
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Recombinant Paraoxonase 1 (PON1) Protein (GST tag). Species: Human. Source: Escherichia coli (E. coli). Order product ABIN4975995.
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Paraoxonase 1 (PON1) activity is markedly influenced by coding polymorphisms, Q/R at position 192 and M/L at position 55 of the PON1 gene. We investigated the frequencies of these polymorphisms and their effects on PON1 and antioxidant activities in 844 South African mixed ancestry individuals. Genotyping was done using allele-specific TaqMan technology, PON1 activities were measured using paraoxon and phenylacetate, oxidative status was determined by measuring the antioxidant activities of ferric reducing antioxidant power and trolox equivalent antioxidant capacity, and lipid peroxidation markers included malondialdehyde and oxidized LDL. The frequencies of Q192R and L55Mwere 47.6% and 28.8%, respectively, and the most common corresponding alleles were 192R (60.4%) and 55M (82.6%).The Q192 was significantly associated with 5.8 units increase in PON1 concentration and 15.4 units decrease in PONase activity after adjustment for age, sex, BMI, and diabetes, with suggestion of differential ...
[4-(4-bromophenyl)phenyl] acetate chemical properties, What are the chemical properties of [4-(4-bromophenyl)phenyl] acetate 84244-98-4, What are the physical properties of [4-(4-bromophenyl)phenyl] acetate ect.
[4-(1-benzothiophen-2-yl)phenyl] acetate 132932-62-8 safety info, [4-(1-benzothiophen-2-yl)phenyl] acetate chemical safety search, Chemical [4-(1-benzothiophen-2-yl)phenyl] acetate safety technical specifications ect.
In recent years, Zr-based metal-organic frameworks (MOFs) have been developed that facilitate catalytic degradation of toxic organophosphate agents, such as chemical warfare agents (CWAs). Because of strict regulations, experiments using live agents are not possible for most laboratories and, as a result, simulants are used in the majority of cases. Reports that employ real CWAs are scarce and do not cover the whole spectrum of agents. We here present a comparative study in which UiO-66-NH2, NU-1000, MOF-808, and PCN-777 are evaluated for their effectiveness in the degradation of paraoxon and the chemical warfare agents tabun, VX, and soman, in N-ethylmorpholine buffer (pH 10) as well as in pure water ...
Characterization and gene cloning of acetylecholinesterase (AChE) in the insecticide-resistant (R) and -susceptible (S) insects have been reported in the past. However, the studies focused mostly on herbivorous pests, rather than predacious species, such as ladybird beetles. Using R and S Propylaea japonica (thunberg), a full-length cDNA sequence (2928 bp) of the ace1-type AChE gene was determined for the first time. The ace1 encoding a protein of 645 amino acids contained typical conserved motifs, such as FGESAG domains, catalytic triad, acyl pocket, oxyanino hole, choline binding site, peripheral anionic site, omega loop and conserved aromatic residues. R P. japonica displayed 50-times greater resistance to chlorpyrifos or mathamidophos with a significantly lower AChE sensitivity to paraoxon, malaoxon, chlorpyrifos or methamidophos than its S counterpart. Five amino acids in the ace1 of R P. japonica differed from those found in S P. japonica. One of them, F358S, located in the acyl-binding ...
Although Pichia pastoris has been successfully used to produce various recombinant heterologous proteins, the efficiency varies. In this study, we used methyl parathion hydrolase (MPH) from Ochrobactrum sp. M231 as an example to study the effect of protein amino acid sequence on secretion from P. pastoris. The results indicated that the protein N-terminal sequence, the endoplasmic reticulum (ER) retention signal (KKXX) at the protein C-terminus, and the acidic stability of the protein could affect its secretion from P. pastoris. Mutations designed based on these sequence features markedly improved secretion from P. pastoris. In addition, we found that the secretion properties of a protein can be cumulative when all of the above strategies are combined. The final mutant (CHBD-DQR) designed by
Carboxylesterases hydrolyze numerous endogenous and foreign compounds with diverse structures. Humans and rodents express multiple forms of carboxylesterases, which share a high degree of sequence identity (∼70%). Alignment analyses locate in carboxylesterases several functional subsites such the catalytic triad as seen in acetylcholinesterase. The aim of this study was to determine among human and rodent carboxylesterases the immunorelatedness, overlapping substrate specificity, differential sensitivity to serine enzyme inhibitors, tissue distribution, and tumor-related expression. Six antibodies against whole carboxylesterases or synthetic peptides were tested for their reactivity toward 11 human or rodent recombinant carboxylesterases. The antibodies against whole proteins generally exhibited a broader cross-reactivity than the anti-peptide antibodies. All carboxylesterases hydrolyzed para-nitrophenylacetate and para-nitrophenylbutyrate. However, the relative activity varied markedly from ...
4-(1-Adamantyl)phenyl acetate | C18H22O2 | CID 269932 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
3-hydroxy-13-amino-13,17-secoandrostan-17-oic-13,17-lactam p-bis(2-chloroethyl)amino phenyl acetate: an alkylating agent for treating breast cancer; lactandrate is the (5alpha)-isomer; structure in first source
Catalysts that are useful for hydrocarbon conversions and oxygenate conversions, and a method for making such catalysts. The method for making the catalysts comprises forming a mixture comprising molecular sieves comprising pores having a diameter smaller than about 10 Angstroms, an inorganic sol, and an external phosphorus source, and drying the mixture.
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PON3兔单克隆抗体[EPR2903(2)](ab109258)可与小鼠, 大鼠, 人样本反应并经WB, IHC实验严格验证。中国75%以上现货,所有产品均提供质保服务,可通过电话、电邮或微信获得本地专属技术支持。
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NTE130 series- Integrated circuit. AM/FM IF. in 7-pin SIP package. Operational temperature range from -15°C to 60°C. from NTE datasheet
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Looking for online definition of organophosphates in the Medical Dictionary? organophosphates explanation free. What is organophosphates? Meaning of organophosphates medical term. What does organophosphates mean?
Paraoxonases are a family of mammalian enzymes with aryldialkylphosphatase activity. There are three paraoxonase isozymes, which were originally discovered for their involvement in the hydrolysis of organophosphates. Research has indicated the enzymatic activity of paraoxonases is more diversified than its activity as an organophosphatase. Esterase and lactonase activity has also been observed from these enzymes and though the physiologically relevant substrates for these enzymes are unknown, it is likely that lactones are the main substrate (although there is a relatively high level of variation in substrate specificity among these enzymes). Most of the studies on the paraoxonase family have specifically looked at the paraoxonase 1 type, leaving much to be learned about the remaining two. The study of this enzyme family has many potential consequences in preventative medicine and toxicology as well as in certain societal contexts. The genes that encode for these enzymes have a number of ...
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Some organophosphorus compounds (OP), including the pesticide mipafox, produce late onset distal axonal degeneration, known as organophosphorus-induced delayed neuropathy (OPIDN). The underlying mechanism involves irreversible inhibition of neuropathy target esterase (NTE) activity, elevated intracellular calcium levels, increased activity of calcium-activated proteases and impaired neuritogenesis. Voltage-gated calcium channels (VGCC) appear to play a role in several neurologic disorders, including OPIDN. Therefore, this study aimed to examine and compare the neuroprotective effects of T-type (amiloride) and L-type (nimodipine) VGCC blockers induced by the inhibitory actions of mipafox on neurite outgrowth and axonal proteins of retinoic-acid-stimulated SH-SY5Y human neuroblastoma cells, a neuronal model widely employed to determine the neurotoxicity attributed to OP ...
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Prolonged exposure to organophosphates in low concentrations caused diarrhoea in 38 students, lecturers and other personnel at an agricultural college.
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A woman and her 3-year-old daughter visiting a relative in Oxon Hill were splashed with a chemical Monday that left them with burns so severe they had to be hospitalized overnight, police and relatives said.
Phenyl phosphonothioic acid-O-ethyl-O-[4-nitrophenyl] ester (EPN) is one of the 10 most frequently used organophosphorus insecticides and causes delayed neurotoxicity in adult chickens and mallards. Small amounts of organophosphorus insecticides placed on birds eggs are embryotoxic and teratogenic. For this reason, the effects of topical egg application on EPN were examined on mallard (Anas platyrhynchos) embryo development. Mallard eggs were treated topically at 72 hr of incubation with 25 microliter of a nontoxic oil vehicle or with EPN in the vehicle at concentrations of approximately 12, 36, or 108 micrograms/g egg, equivalent to one, three, and nine times the agricultural level of application used to spray crops. Treatment with EPN resulted in 22 to 44% mortality over this dose range by 18 days of development compared with 4 and 5% for untreated and vehicle-treated controls. EPN impaired embryonic growth and was highly teratogenic: 37-42% of the surviving embryos at 18 days...
The inhibition of acetylcholinesterase in the presence of selected organothiophosphates (diazinon, malathion, chlorpyrifos, azinphos-methyl, phorate) and their oxo-analogues (diazoxon, malaoxon, chlorpyrifos-oxon, azinphos-methyl-oxon, phorate-oxon) was examined. Experimental conditions were optimized to detect the lowest posible concentrations of these compounds using AChE test. IC50 values were determined for all the mentioned compounds. Investigated organothiophosphates have been converted into their oxo-analogues in the presence of the enzyme myeloperoxidase. Oxidation products were detected using UPLC and GC/MS analysis. It was found that the products are stable within minimum 1h. In order to optimize oxidation procedure and achieve maximum concentrations of oxons, the optimal concentrations of H2O2 (50 μM) and MPO (100 nM) were determined. Also, the optimal incubation time of OPs and MPO (10 min), as well as the optimal pH (6) and temperature (25 °C) were estimated. Oxidation of ...
The objective of this investigation was to determine the distribution of cholinergic (acetyl-cholinesterase, AChE) and noncholinergic markers in slow-, fast-, and mixed-fiber containing muscles (soleus, SOL; extensor digitorum longus, EDL; and diaphragm, DIA, respectively). Noncholinergic markers included high-energy phosphates (adenosine triphosphate, ATP; phosphocreatine, PCr; and their metabolites), and the activity of creatine kinase (CK) and lactate dehydrogenase (LDH) and their isoenzymes and subforms. All three types of muscles had only one CK isoenzyme, CK-MM, which totally consisted of MM3 subform. Levels of these determinants were highest in EDL followed by DIA and least in SOL. Another objective was to determine alterations of these markers under the influence of acute carbofuran (1.5 mg/kg) or methyl parathion (MPTH, 5 mg/kg) toxicity. Rats receiving either insecticide showed cholinergic signs with maximal severity including muscle fasciculations and convulsions within 15-30 min that lasted
GC Application #18326: European Organophosphorous Pesticides Mix # 1 on ZB-5MSi. Column used: Zebron™ ZB-5MSi, GC Cap. Column 30 m x 0.25 mm x 0.25 µm, Ea Part#: 7HG-G018-11
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Measurement of Carboxylesterase (CES) Activities (Masakiyo Hosokawa, Chiba University, Chiba, Japan and Tetsuo Satoh, Biomedical Research Institute, Chiba, Japan)
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Acetylcholinesterase小鼠单克隆抗体[HR2](ab2803)可与小鼠, 兔, 豚鼠, 牛, 猫, 人, 猕猴样本反应并经IP, ELISA, IHC, Flow Cyt, ICC/IF实验严格验证,被3篇文献引用。
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乙醯膽鹼酯酶[1](英語:Acetylcholinesterase,簡稱為AChE,EC 3.1.1.7)是一種降解(通過其水解活性)神經遞質乙醯膽鹼成為膽鹼和乙酸的酶。該酶主要存在於神經肌肉接頭與膽鹼能神經系統中,在這些地方該酶的活性就是為了終止突觸傳遞。乙醯膽鹼酯酶具有極高的水解活性--每秒鐘一分子的乙醯膽鹼酯酶可以水解25000分子的乙醯膽鹼。經乙醯膽鹼酯酶作用而產生的膽鹼被重新利用--通過重攝取被轉運進入神經末梢,在那裡被重新利用以合成新的乙醯膽鹼分子[2]。. ...
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Acute neurotoxic effects during the cholinergic phase of organophosphorus insecticide poisoning and delayed neurotoxic effects appearing two to three weeks later are well recognized. We observed 10 patients who had paralysis of proximal limb muscles,
Human plasma paraoxonase (PON1) has been shown to have arylesterase and paraoxonase activity. This high-density lipoprotein (HDL) associated enzyme exhibits antiatherogenic properties and acts as a detoxifying agent for several chemical warfare agents and insecticides. We show that the reported purification process (Gan et al.) contains a ~68kDa co-purifying contaminant. We have developed a modified procedure using size exclusion chromatography to obtain pure PON1 from human serum. In order to support the current homology model of PON1 developed using the crystal structure of DFPase as a model, a CD spectrum of pure, monodisperse PON1 was measured. Previous attempts were inconclusive due to a high background caused by detergent micelle light scattering. The detergent free form of PON1 has been characterized to exist as monomer, dimer, and higher order soluble aggregates. Thus, detergents are necessary to retain native, monodisperse enzyme. In conjunction with our modified purification procedure, ...
Although pesticide-bound AChE undergoes hydrolytic regeneration at a very slow rate, this process can be enhanced by using an oxime medication such as pralidoxime hydrochloride (2-PAM). Pralidoxime is unable to rejuvenate active enzyme from the OP-AChE complex that has undergone aging. Therefore, pralidoxime therapy is most effective if started early in the course of toxicity. The starting dose of pralidoxime for adults is 1-2 g IV and for children 20-40 mg/kg IV, both over 10-15 minutes. A constant infusion of pralidoxime appears to be more effective than bolus dosing in maintaining necessary levels. For adults, a maintenance infusion of 250-500 mg/h is usually recommended, titrating to symptoms, but infusions of up to 8 mg/kg/h or more may be required in some cases. Reports in children suggest using a continuous infusion of 10-20 mg/kg/h after the initial bolus. Side effects of pralidoxime are usually minimal at normal doses. The efficacy of pralidoxime in some anticholinesterase pesticide ...
ECHAs dossier evaluation process covers compliance checks and the examination of testing proposals. By consulting the table below, you can find out whether ECHA has started to evaluate dossiers for a particular substance and follow the progress through the evaluation process. The table below displays the type, scope and status of the assessment undertaken for a given dossier. The decision date and the non-confidential version of the decision are published shortly after the decision has been adopted. Before publishing the non-confidential version of an adopted decision on its website, ECHA consults the addressees of the decision on this version. ECHA systematically removes any personal data from the non-confidential version of a decision. Some sections may also be redacted based on justified claims by registrants, regarding information confidential or deemed to harm their commercial interest if disclosed. Check the expandable boxes below for more details. ...
Organophosphate poisoning in children - How can organophosphate poisoning be treated? Decontaminate. Atropine injection as soon as possible. Followed by supportive care. Person might need ventilator support for breathing until effects of OP provisioning wears off.
Nerve agents are compounds that have the capacity to inactivate the enzyme acetylcholinesterase (AChE). The first compounds to be synthesized were known as the G-series agents (
Organophosphates and carbamates are the most frequently used insecticides worldwide. These compounds cause 80% of the reported toxic exposures to insecticides.
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Dr. Walsh responded: Inhibits AChE. Organophosphates inhibit acetocholinesterase, which is responsible for recycling actetocholine. This leads to muscle overstimulation and rigid |a href="/topics/paralysis" track_data="{
Exposure to organophosphates has acute effects on health, but evidence of chronic effects is unclear. Many people who have been occupationally exposed
PR firms no-bid deal scrutinized (3/12)Pesticide maker a generous political donor (3/08)Q&A on chemical CheckMate (2/23)Bills aimed to curb moth eradication pr. LEARN ABOUT THIS ...
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Mintisal (Paraoxon)Mintisal (Paraoxon)

Mintisal information about active ingredients, pharmaceutical forms and doses, Mintisal indications, usages and related health products lists
more infohttp://drugs-about.com/drugs-m/mintisal.html

Paraoxon - WikipediaParaoxon - Wikipedia

Paraoxon has been used by scientists to study acute and chronic effects of organophosphate intoxication. It is easily absorbed ... Paraoxon is one of the most potent acetylcholinesterase-inhibiting insecticides available, around 70% as potent as the nerve ... Paraoxon is a parasympathomimetic which acts as an acetylcholinesterase inhibitor. It is an organophosphate oxon, and the ... NTI Country Overviews:South Africa:Chemical Capabilities:Paraoxon. ...
more infohttps://en.wikipedia.org/wiki/Paraoxon

Molecules | Free Full-Text | Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase...Molecules | Free Full-Text | Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase...

... which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. In case of BuChE ... inhibited by paraoxon. Their reactivation activity was compared with standard reactivators-pralidoxime, obidoxime and HI-6- ... Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon. Kamil Kuca 1, ... "Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Paraoxon." Molecules 14 ...
more infohttp://www.mdpi.com/1420-3049/14/12/4915

NIOSHTIC-2  Publications Search - 20025200 - Comparison of chlorpyrifos-oxon and paraoxon acetylcholinesterase inhibition...NIOSHTIC-2 Publications Search - 20025200 - Comparison of chlorpyrifos-oxon and paraoxon acetylcholinesterase inhibition...

Comparison of chlorpyrifos-oxon and paraoxon acetylcholinesterase inhibition dynamics: potential role of a peripheral binding ... and paraoxon (PO) concentrations (0.5 pM -100 nM) using the Ellman assay combined with a dynamic model. The results indicated ...
more infohttps://www.cdc.gov/niosh/nioshtic-2/20025200.html

Cholinesterase activity of muscle tissue from freshwater fishes: Characterization and sensitivity analysis to the methyl...Cholinesterase activity of muscle tissue from freshwater fishes: Characterization and sensitivity analysis to the methyl...

... paraoxon organophosphate. The biochemical characterization of cholinesterases (ChE) from different teleost species has be... ... Moreover, muscle tissues ChE sensitivity to methyl‐paraoxon (MP) organophosphate (OP) pesticide was evaluated by determining ... paraoxon organophosphate. Be the first to comment! ...
more infohttps://www.environmental-expert.com/articles/cholinesterase-activity-of-muscle-tissue-from-freshwater-fishes-characterization-and-sensitivity-ana-419278

Comparing Therapeutic and Prophylactic Protection against the Lethal Effect of Paraoxon : Toxicological Sciences - oiComparing Therapeutic and Prophylactic Protection against the Lethal Effect of Paraoxon : Toxicological Sciences - oi

LD50 of paraoxon with antagonists)/0.9 mg/kg (LD50 of control paraoxon)]. The current study firmly establishes the value of ... LD50 of paraoxon with antagonists)/ 0.95 mg/kg (LD50 of control paraoxon)], and the therapeutic antidotal protection was 156 LD ... Keywords: organophosphorus hydrolase (OPH); OPA anhydrase; paraoxonase; paraoxon antagonism; sterically stabilized liposomes; ... in paraoxon poisoning. Prophylactic and therapeutic properties of atropine and 2-PAM are diminished when they are used alone. ...
more infohttp://oxfordindex.oup.com/view/10.1093/toxsci/kfg185

Anxiety-related Behavioral Alterations Following Repeated Paraoxon Exposure in Rats -  Journal of Mazandaran University of...Anxiety-related Behavioral Alterations Following Repeated Paraoxon Exposure in Rats - Journal of Mazandaran University of...

Plasma and brain ChE activity was inhibited in a dose dependent manner by paraoxon. Paraoxon (0.3 mg/kg) increased the ... Materials and methods: Adult male Wistar rats were repeatedly exposed to paraoxon at daily doses of 0.1, 0.2, and 0.3 mg/kg, IP ... The purpose of this study was to investigate the influence of repeated exposure to paraoxon on behaviors related to anxiety in ... Mohammadi M, Parsi B. Anxiety-related Behavioral Alterations Following Repeated Paraoxon Exposure in Rats. J Mazandaran Univ ...
more infohttp://jmums.mazums.ac.ir/article-1-4453-en.html

Optical Detection of Paraoxon Using Single-Walled Carbon Nanotube Films with Attached Organophosphorus Hydrolase-Expressed...Optical Detection of Paraoxon Using Single-Walled Carbon Nanotube Films with Attached Organophosphorus Hydrolase-Expressed...

Optical Detection of Paraoxon Using Single-Walled Carbon Nanotube Films with Attached Organophosphorus Hydrolase-Expressed ... Paraoxon was hydrolyzed using this device, and detected by measuring the concentration of the enzymatic reaction product, p- ... Optical Detection of Paraoxon Using Single-Walled Carbon Nanotube Films with Attached Organophosphorus Hydrolase-Expressed ... Optical Detection of Paraoxon Using Single-Walled Carbon Nanotube Films with Attached Organophosphorus Hydrolase-Expressed ...
more infohttp://libros.duhnnae.com/2017/jun6/149757666471-Optical-Detection-of-Paraoxon-Using-Single-Walled-Carbon-Nanotube-Films-with-Attached-Organophosphorus-Hydrolase-Expressed-Escherichia-coli.php

High-Resolution Crystal Structure of Plant Carboxylesterase AeCXE1, fromActinidia eriantha, and Its Complex with a High...High-Resolution Crystal Structure of Plant Carboxylesterase AeCXE1, fromActinidia eriantha, and Its Complex with a High...

AeCXE1 was also found to be inhibited by organophosphates, with paraoxon (IC50 = 1.1 muM) a more potent inhibitor than ... and Its Complex with a High-Affinity Inhibitor Paraoxon†,‡ Academic Article * View record in Web of Science ® ... dimethylchlorophosphate (DMCP; IC50 = 9.2 muM). The structure of AeCXE1 with paraoxon bound was determined at 2.3 A resolution ...
more infohttps://scholars.latrobe.edu.au/display/publication71247

Pyrimidifen 10 µg/mL in Acetonitrile- CAS Number 105779-78-0Pyrimidifen 10 µg/mL in Acetonitrile- CAS Number 105779-78-0

Paraoxon-ethyl. 100 mg. DRE-C15850000. Add to basket Paraoxon-ethyl 10 µg/mL in Cyclohexane. 10 mL. DRE-L15850000CY. Add to ... Paraoxon-ethyl 100 µg/mL in Cyclohexane. 1 mL. DRE-XA15850000CY. Add to basket ... Paraoxon-methyl 10 µg/mL in Isooctane. 10 mL. DRE-L15860000IO. Add to basket ...
more infohttps://www.lgcstandards.com/PL/en/Pyrimidifen-10-g-mL-in-Acetonitrile/p/DRE-L16659300AL

Phenthoate 10 µg/mL in Isooctane- CAS Number 2597-03-7Phenthoate 10 µg/mL in Isooctane- CAS Number 2597-03-7

Paraoxon-ethyl. 100 mg. DRE-C15850000. Add to basket Paraoxon-ethyl 10 µg/mL in Cyclohexane. 10 mL. DRE-L15850000CY. Add to ... Paraoxon-ethyl 100 µg/mL in Cyclohexane. 1 mL. DRE-XA15850000CY. Add to basket ... Paraoxon-methyl 10 µg/mL in Isooctane. 10 mL. DRE-L15860000IO. Add to basket ...
more infohttps://www.lgcstandards.com/PL/en/Phenthoate-10-g-mL-in-Isooctane/p/DRE-L16050000IO

IJMS  | Free Full-Text | Genomic and Phenotypic Alterations of the Neuronal-Like Cells Derived from Human Embryonal Carcinoma...IJMS | Free Full-Text | Genomic and Phenotypic Alterations of the Neuronal-Like Cells Derived from Human Embryonal Carcinoma...

... paraoxon, are able to alter differentiation of neural precursor cells in vitro. Exposure to 1 µM paraoxon (non-cytotoxic ... We conclude that 1 µM paraoxon could affect the initial stage of in vitro neurodifferentiation possibly due to a teratogenic ... activity resistant to paraoxon and sensitive to mipafox. B (paraoxon-resistant) and C activity (resistant to both paraoxon and ... Effect of Paraoxon and Mipafox on NTE Activity. Non-neuropathic OP paraoxon did not inhibit NTE after 4, 10 or 15 days of ...
more infohttp://www.mdpi.com/1422-0067/15/1/905/htm

Zeitschrift für Naturforschung CZeitschrift für Naturforschung C

Cooperative Binding of the Organophosphate Paraoxon to the (Na+ + K+)-ATPase. Blasiak, Janusz ...
more infohttps://www.degruyter.com/view/j/znc.1995.50.issue-9-10/issue-files/znc.1995.50.issue-9-10.xml

Academic JournalsAcademic Journals

The limit of detection for beverages ranged from 32 to 48 ppb corresponding to 0.32-0.48 ng of paraoxon in absolute values. The ... The measuring protocol was based on inhibition of the enzyme acetylcholinesterase by paraoxon that resulted in decreased or no ... Multichannel spectrophotometry for analysis of organophosphate paraoxon in beverages Authors: MIROSLAV POHANKA, JANA ZDAROVA ... Abstract: Multichannel spectrophotometry was performed to assay for paraoxon in spiked beverages. A 96-well microplate was used ...
more infohttp://journals.tubitak.gov.tr/chem/abstract.htm?id=10681

Ghent University Academic BibliographyGhent University Academic Bibliography

Neuropathological characteristics of paraoxon and fenthion myopathy Jan De Bleecker (UGent) , S DE PRAETERE, Patrick Santens ( ...
more infohttps://biblio.ugent.be/publication?q=parent+exact+%22Neurology%22&limit=250

Biotransformation of Parathion in Human Liver: Participation of CYP3A4 and its Inactivation during Microsomal Parathion...Biotransformation of Parathion in Human Liver: Participation of CYP3A4 and its Inactivation during Microsomal Parathion...

The separation of parathion, paraoxon and 4-nitrophenol on Ultrasphere-Si (5 μm, 4.6 mm i.d × 25 cm; Beckman, San Ramon, CA) ... In human hepatic microsomal fractions, the ratio of 4-nitrophenol to paraoxon formation was 1.12 ± 0.06 (table 1). Of the three ... Further, paraoxon and 4-nitrophenol were noninhibitory toward 7-ethylresorufin O-deethylation activity (not shown). ... As shown in table 1, the individual variation in parathion (250 μM) oxidation to paraoxon and 4-nitrophenol was considerable ( ...
more infohttp://jpet.aspetjournals.org/content/280/2/966?ijkey=4fc647d9702b88d19f7375efc71323815e761d34&keytype2=tf_ipsecsha

Miroslav Pohanka - NeL.eduMiroslav Pohanka - NeL.edu

Mixture toxicity of microcystin-LR, paraoxon and bromadiolone in Xenopus laevis embryos.. Ondracek K, Bandouchova H, ... paraoxon and bromadiolone in Xenopus laevis embryos. Neuro Endocrinol Lett. 2015 Jan; 36(Suppl 1): 114-119 ...
more infohttp://www.nel.edu/pohanka-90/?vp-page=1

Hana Bandouchova - NeL.eduHana Bandouchova - NeL.edu

Mixture toxicity of microcystin-LR, paraoxon and bromadiolone in Xenopus laevis embryos.. Ondracek K, Bandouchova H, ... paraoxon and bromadiolone in Xenopus laevis embryos. Neuro Endocrinol Lett. 2015 Jan; 36(Suppl 1): 114-119 ...
more infohttp://www.nel.edu/bandouchova-128/

NIOSHTIC-2  Publications Search - 00182915 - Preliminary Results from a Regional Comparison of Insecticide Decay.NIOSHTIC-2 Publications Search - 00182915 - Preliminary Results from a Regional Comparison of Insecticide Decay.

Paraoxon (311455) levels were also low. Very similar results were obtained in Arizona, with the exception that there were ... Parathion decays very rapidly from apple leaves, reaching approximately zero after 14 days with paraoxon levels reaching ... When comparing apple leaves and grape leaves in California, more paraoxon was found on grape leaves. ... California orange leaves had more paraoxon on the surface than Arizona orange leaves. ...
more infohttps://www.cdc.gov/niosh/nioshtic-2/00182915.html

ATC 코드 S01 - 위키백과, 우리 모두의 백과사전ATC 코드 S01 - 위키백과, 우리 모두의 백과사전

S01EB10 Paraoxon. S01EB51 Pilocarpine, combinations. S01EB58 Aceclidine, combinations. S01EC 탄산무수화효소 저해제[편집]. S01EC01 ...
more infohttps://ko.wikipedia.org/wiki/ATC_%EC%BD%94%EB%93%9C_S01

Cholinesterase Inhibitors - DrugBankCholinesterase Inhibitors - DrugBank

Paraoxon. Not Available. DB01381. Ginkgo biloba. Appears to be effective in: alleviating age-related memory impairment in some ...
more infohttps://www.drugbank.ca/categories/DBCAT000815

Alclometasone - DrugBankAlclometasone - DrugBank

Paraoxon. The risk or severity of adverse effects can be increased when Alclometasone is combined with Paraoxon.. Experimental ...
more infohttps://www.drugbank.ca/drugs/DB00240
  • Studies in rat liver have shown that cytochrome P450 (CYP) enzymes mediate the oxidative biotransformation of the phosphorothioate pesticide parathion to paraoxon and 4-nitrophenol. (aspetjournals.org)
  • While it was difficult to make a comparison to California data, as a much less concentrated solution of parathion was applied there, California orange leaves had more paraoxon on the surface than Arizona orange leaves. (cdc.gov)
  • Parathion decays very rapidly from apple leaves, reaching approximately zero after 14 days with paraoxon levels reaching similar lows. (cdc.gov)
  • Studies on the Percutaneous Absorption of Parathion and Paraoxon. (epa.gov)
  • Parathion in the air is rapidly transformed by sunlight and ozone into a degradation product, paraoxon, a substance more toxic than parathion. (cdc.gov)
  • Therefore, the objective of the current study was to evaluate the in vitro inhibition of AChE by a wide range of chlorpyrifos oxon (CPO) and paraoxon (PO) concentrations (0.5 pM -100 nM) using the Ellman assay combined with a dynamic model. (cdc.gov)
  • We conclude that 1 μM paraoxon could affect the initial stage of in vitro neurodifferentiation possibly due to a teratogenic effect, while the absence of transcriptional alterations by mipafox exposure did not allow us to conclude a possible effect on neurodifferentiation pathways at the tested concentration. (mdpi.com)
  • Mixture toxicity of microcystin-LR, paraoxon and bromadiolone in Xenopus laevis embryos. (nel.edu)
  • Exposure to 1 μM paraoxon (non-cytotoxic concentrations) altered the expression of different genes involved in signaling pathways related to chromatin assembly and nucleosome integrity. (mdpi.com)
  • Materials and methods: Adult male Wistar rats were repeatedly exposed to paraoxon at daily doses of 0.1, 0.2, and 0.3 mg/kg, IP for 14 days. (ac.ir)
  • Prophylactic and therapeutic efficacy against organophosphorus (OP) intoxication by pralidoxime (2-PAM) and atropine were studied and compared with sterically stabilized long-circulating liposomes encapsulating recombinant organophosphorus hydrolase (OPH), either alone or in various specific combinations, in paraoxon poisoning. (oup.com)
  • As it resulted, none of the prepared compounds surpassed obidoxime, which is considered to be the most potent compound if used for reactivation of AChE inhibited by paraoxon. (mdpi.com)
  • The purpose of this study was to investigate the influence of repeated exposure to paraoxon on behaviors related to anxiety in male adult rats. (ac.ir)
  • Paraoxon was hydrolyzed using this device, and detected by measuring the concentration of the enzymatic reaction product, p-nitrophenol. (duhnnae.com)
  • In water, reaction with other chemicals and with sunlight produces paraoxon. (cdc.gov)
  • Results: Plasma and brain ChE activity was inhibited in a dose dependent manner by paraoxon. (ac.ir)