Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Electrophysiological experiments were done to investigate the effect o p-nitrophenyl diazonium fluoroborate (p-NPD) on motor endplates of the frog's m. cutaneus pectoris. The compound has no direct depolarizing effect on the postsynaptic membrane and stabilizes it irreversibly when added to the bath. Longtime iontophoretical applications of p-NPD produce a biphasic effect: initially a potentiation of the depolarizations due to acetylcholine (ACh) (both iontophoretically applied and presynaptically liberated), and subsequently an inhibition of the response to ACh. When the acetylcholinesterase (AChE) is inactivated previously, only the inhibiting effect of the compound is demonstrable. The association constant of p-NPD to purified AChE and to membrane fragments of electroplax was determined by biochemical methods. The compound's affinity to the AChE was found to be about 20 times greater than to the acetylcholine receptor (AChR). Iontophoretical application of p-NPD to cholinergic neurons in the hippocampal cortex of the cat also produced the characteristic biphasic effect on ACh-induced activity of these investigated neurons. The results suggest that the biphasic effect depends on the capacity of p-NPD to combine with both the AChE and the AChR. The AChE is first inhibited with low concentrations thereby potentiating the ACh response. At higher concentrations the AChR's are progressively inhibited too, thereby diminishing the excitability of the postsynaptic membrane up to a complete block.
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PMID:Effect of p-nitrophenyl diazonium fluoroborate on cholinergic mechanisms. 108 74

A death due to ingestion of 2,4-dichlorophenoxyacetic acid (2,4-D), 2-(2-methyl-4-chlorophenoxy) propionic acid (MCPP), and phosphorothioic acid O,O-diethyl O-(3,5,6-trichloro-2-pyridinyl)ester (chlorpyrifos) is reported. The clinical course, dose ingested, and plasma levels of the chemicals were compatible with previous fatalities due to the chlorophenoxyacetic acids. Chlorpyrifos concentrations and tissue cholinesterase and in esterase inhibitions indicated the presence of the organophosphate and its biochemical effect, but few cholinergic signs were observed clinically. Lymphocytic neurotoxic esterase activity was decreased for a limited period of time after ingestion. Postmortem nervous tissue neurotoxic esterase was also decreased. This association has not been demonstrated before in man. HPLC and GC/NPD methods for measuring chlorophenoxy acetic acids and chlorpyrifos, respectively, are presented.
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PMID:Toxicologic studies in a fatal overdose of 2,4-D, MCPP, and chlorpyrifos. 619 35

Succinylcholine, a bis-quaternary ammonium compound, is considered an elusive analyte due to rapid hydrolysis by pseudocholinesterase in plasma. However, tissue acetylcholinesterase is relatively inactive toward this substrate. Hence, analysis of tissues of succinylcholine-treated animals may reveal the presence of unchanged drug. This report describes three chromatographic techniques (TLC, GC/NPD, and GC/MS) which may be applied to the analysis of this substance in human tissues. Validation of the techniques was accomplished using tissues from rats treated with succinylcholine.
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PMID:Determination of succinylcholine in tissues by TLC, GC/NPD, and GC/MS. 664 6

Human serum paraoxonase (PON1) and perhaps other mammalian paraoxonases catalyzes the hydrolysis of certain organophosphorus (OP) insecticides and nerve gases and so may alter significantly an individual's susceptibility to the toxicity of these chemicals. Serum PON1 exhibits a substrate dependent polymorphism and this polymorphism shows great interethnic variability. This study focused on the investigation of PON1, arylesterase and cholinesterase activities in 28 acute OP insecticide poisoning cases. Insecticide analysis were performed by GC-NPD and activities of enzymes were measured by using spectrophotometer. The activity levels for salt stimulated PON1, basal PON1 and arylesterase were found as 78.83 (35.39-186.13), 39.97 (2.49-80.43) micromol/min/l and 126.26 (36.34-288.24) mmol/min/l respectively. On the other hand the activity levels for butyrylcholinesterase (BTC) and acetylcholinesterase (AchE) were found as 797.23 (106.3-3823)U/l and 4.65 (0.21-30.29)U/ml. There was a correlation between percent stimulation of PON1 and BTC activities (r=0.446, P<0.05), but this correlation was lower than in cases who exposed to OP insecticides chronically. As a conclusion, in chronic and acute OP exposure, both PON1 level and phenotype must be taken into consideration.
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PMID:Human serum paraoxonase (PON1) activity in acute organophosphorous insecticide poisoning. 1274 1

The study aimed to determine the hazardous health effects of pesticides exposure in the factory workers by measuring plasma cholinesterase (PChE), pesticides residues, and renal and hepatic biochemical markers. In addition, we also assessed the knowledge, attitudes, and safety practices adopted by the industrial workers. The study was conducted in three different sizes of factories located in Lahore (large), Multan (medium), and Karachi (small) in Pakistan. Total 238 adult males consisting of 184 pesticide industrial workers (exposed group) from large-sized (67), medium-sized (61), small-sized (56) industrial formulation factories, and 54 controls (unexposed) were included in the study. All the participants were male of aged 18 to 58 years. PChE levels were estimated by Ellmann's method. Plasma pesticides residue analysis was performed by using reverse phase C-18 on high-performance liquid chromatograph and GC with NPD detector. Plasma alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine, urea, and gamma glutamyltransferase (GGT) were measured on Selectra E auto analyzer. Plasma and C-reactive protein was analyzed by Immulite 1000. The results revealed a significant decrease in plasma post exposure PChE levels (<30%) as compared to baseline in the workers of small (29%) and medium (8%) industrial units (p < 0.001). Plasma cypermethrin, endosulfan, imidacloprid, thiodicarb, carbofuran, and methamidophos levels were found to be higher than allowable daily intake. Serum AST, ALT, creatinine GGT, malondialdehyde, total antioxidant, and CRP were significantly raised among the workers of small and medium pesticide formulation factories as compared to large industrial unit and controls (p < 0.001). The study demonstrated that unsafe practices among small- and medium-sized pesticides industrial workers cause significant increase in pesticide exposure, oxidative stress, and derangement of hepatic and renal function.
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PMID:Monitoring health implications of pesticide exposure in factory workers in Pakistan. 1966 82