Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.1.8 (cholinesterase)
12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The kinetics of cholinesterase enzymatic hydrolysis of carboxylic acid adamantyl derivatives was studied in vitro. The maximal rate of enzymatic hydrolysis in the series of bis-esters was shown to increase on elongation of the distance between ester groups. The maximal hydrolysis rate in the series of bis- and mono-esters decreases on elongation of the distance between ester group and quaternary nitrogen atom. The addition of adamantyl radical to the alcohol part of the molecule of bis- and mono-esters prevents the hydrolysis. The addition of lipophilic radicals to the cationic group of derivatives of mono- and dicarboxylic acids exerts a greater effect on the maximal hydrolysis rate in monoesters than in bis-esters.
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PMID:[Hydrolysis by plasma cholinesterase of complex adamantyl-containing esters]. 323 39

Benzoic acid esters of various substituted 2-hydroxyacetamides (glycolamides) were found to be hydrolyzed extremely rapidly in human plasma solutions, the half-lives of hydrolysis being less than 5 s in 50% plasma solutions for some N,N-disubstituted glycolamide esters. The rapid rate of hydrolysis could be largely attributed to cholinesterase (also called pseudocholinesterase) present in plasma. From a study of a variety of substituted glycolamide esters and structurally related esters, the most prominent structural requirement needed for a rapid rate of hydrolysis was found to be the glycolamide ester structure combined with the presence of two substituents on the amide nitrogen atom. A structural similarity of such esters with benzoylcholine, a good substrate for cholinesterase, was put forward. Esters of N,N-disubstituted glycolamides are suggested to be a useful biolabile prodrug type for several carboxylic acid agents. The esters combine a high susceptibility to undergo enzymatic hydrolysis in plasma with a high stability in aqueous solution. Furthermore, as demonstrated with the benzoic acid model esters, it is feasible to obtain ester derivatives with almost any desired water solubility or lipophilicity with retainment of marked lability to enzymatic hydrolysis.
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PMID:Glycolamide esters as biolabile prodrugs of carboxylic acid agents: synthesis, stability, bioconversion, and physicochemical properties. 337 86

F344/N rats and B6C3F1 mice were exposed to 0, 1, 3, or 6 ppm methyl isocyanate by inhalation for 6 hr on 4 consecutive days. Deaths of rats were observed following 3 ppm exposures, and mice died after exposures to 6 ppm. Deaths appeared to be related to severe respiratory distress. Survivors in high dose groups lost weight initially, then gained weight at rates equal to controls throughout a 91-day recovery period. Lung weights increased significantly in male and female rats exposed to 3 ppm, but no persistent changes in brain, kidney, thymus, spleen, liver, or testis weights were seen in either mice or rats. Blood and serum from male and female rats were taken for clinical pathology and hematology assessments on day 7 of postexposure, the day prior to the first observed deaths of these animals. No changes or only slight changes were seen in measures of serum alanine aminotransferase, sorbitol dehydrogenase, alkaline phosphatase, or in blood and brain cholinesterase activities. However, serum creatine kinase increased with dose in both males and females. Blood urea nitrogen, creatinine, and methemoglobin were unchanged. No changes were seen in counts of red blood cells or platelets, or in red cell indices. Hemoglobin concentrations and hematocrits were slightly elevated. No changes were noted in absolute leukocyte counts, but counts of segmented neutrophils increased and lymphocytes decreased.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:The toxicity of inhaled methyl isocyanate in F344/N rats and B6C3F1 mice. II. Repeated exposure and recovery studies. 362 27

1. A variety of biochemical measurements were taken periodically in captive northern bobwhite (Colinus virginianus L.), European starlings (Sturnus vulgaris L.), red-winged blackbirds (Agelaius phoeniceus L.) and common grackles (Quiscalus quiscula L.) to determine whether baseline values remain sufficiently stable throughout the year for general clinical use in the absence of concurrent control specimens. 2. Variables included whole blood hematocrit and hemoglobin, plasma lactate dehydrogenase, alpha-hydroxybutyrate dehydrogenase, aspartate aminotransferase, alanine aminotransferase, creatine kinase, butyrylcholinesterase, alkaline phosphatase, glucose, albumin, total protein, creatinine, urea nitrogen, uric acid, cholesterol, and triglycerides, and brain acetylcholinesterase. Butyryl- and acetylcholinesterase were included because of their specific uses in toxicology. 3. Significant seasonal differences were detected for each of the variables except brain acetylcholinesterase in at least one of the species. Significant species differences were detected during at least one season for all of the variables measured. 4. All species were maintained outdoors, but only northern bobwhites came into reproductive condition and showed sex-differences in the clinical variables during their normal breeding season. 5. It was concluded that reference values for the 18 clinical variables measured could be calculated from our data for adult specimens of the species studied, and that results for one species cannot be extrapolated with certainty to any other species. 6. Estimated normal bounds for each of the 18 variables measured by commonly used clinical procedures are presented for reproductively quiescent northern bobwhites, European starlings, red-winged blackbirds, and common grackles.
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PMID:Seasonal variation in diagnostic enzymes and biochemical constituents of captive northern bobwhites and passerines. 366 39

Changes in the amount of hippurate synthesized and excreted in the urine after 1.5 gm benzoate loading (intravenous hippuric acid test [HAT]) in patients with liver disease before surgery were studied in relation to arterial blood ketone body ratio (acetoacetate/beta-hydroxybutyrate) (BKBR), reflecting energy status of the liver. In these patients, the HAT values for 120 minutes were decreased significantly (1.088 +/- 0.129 gm, n = 9; 1.071 +/- 0.258 gm, n = 7; 1.258 +/- 0.126 gm, n = 10; in cirrhosis with liver tumor, cirrhosis with esophageal varix, and obstructive jaundice, respectively) as compared with the value in patients without liver disease (1.829 +/- 0.093 gm, n = 16, P less than 0.01). The correlation coefficient of the BKBR and the HAT value was 0.766, which was higher than that of the BKBR and albumin or the BKBR and choline esterase (r = 0.532 and r = 0.646, respectively). Serum levels of glutamic-oxaloacetic transaminase, glutamic pyruvic transaminase, alkaline phosphatase, gamma-glutamyl transpeptidase, leucine aminopeptidase, total and direct bilirubin, creatinine, and blood urea nitrogen were not correlated with the HAT values. Because hippurate is synthesized in liver mitochondria by the continuous supply of adenosine triphosphate through mitochondrial oxidative phosphorylation, HAT is considered to be a test that evaluates the energetic capacity of the liver to manage a metabolic load imposed on it.
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PMID:Clinical significance of hippurate-synthesizing capacity in surgical patients with liver disease: a metabolic tolerance test. 377 26

Eight hematologic parameter values, 16 serum biochemical constituents, serum protein fractions and albumin-globulin ratios were determined in blood samples obtained from 879 normal, healthy Beagle dogs of both sexes which had been reproduced and bred in our laboratories. The blood samples were collected from the Beagles that ranged in monthly ages from 1 to 12 and in monthly ages from 13 to 121, which were classified as the adult class. As a result, red blood cell counts, hemoglobin concentrations and packed cell volumes increased with growth. Red blood cell parameters of normal Beagles in our laboratories were rather higher than those in literatures presented by many other researchers. MCV decreased and MCHC increased gradually with age. Total serum protein concentrations increased with growth. alpha 1-1 and alpha 1-2 Globulin fractions descended, but beta 2 and gamma globulin fractions ascended in serum proteins. Alkaline phosphatase activities, inorganic phosphorus concentrations and glucose concentrations decreased conspicuously with growth. Leucine aminopeptidase activities and calcium concentrations decreased slightly. Serum cholinesterase and LDH activities showed a tendency to diminish similarly. Blood urea nitrogen and creatinine concentrations multiplied gradually. Hematologic parameters became almost steady in our 7-month-old dogs or older ones and serum biochemical constituents had a tendency to be stable in our 7- to 9-month-old dogs or older ones in the blood. White blood cell counts, alkaline phosphatase activities, inorganic phosphorus concentrations, glucose concentrations, leucine aminopeptidase activities and calcium concentrations were lowest in the adult class.
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PMID:[Successive changes in the blood composition of experimental normal beagle dogs associated with age]. 408 64

1. The second-order rate constants of inhibition, k(a), of acetylcholinesterase were measured at pH values between 5.5 and 10.5 for two esters of phosphorus acids and five esters of carbamic acids. Two of the carbamates and one of the phosphates contained a quaternary nitrogen group. 2. For the three positively charged compounds the k(a)-pH plots are bell-shaped, with a pH optimum between 7.5 and 9.0. The changes in k(a) above and below the optimum pH fit theoretical curves for the dissociation of groups on the protein of pK 6.2 and 10.25. 3. For the uncharged compounds, the k(a)-pH plot on the alkaline side is identical with the one obtained for charged inhibitors. On the acid side they do not fit such a curve and the k(a) for two of the carbamates is independent of pH changes between 5.5 and 8.0. 4. The first-order rate constants, k(+3), for spontaneous reactivation were measured at pH values between 5.0 and 11.0 for N-methylcarbamoylated, NN-dimethylcarbamoylated and di-(2-chloroeth)phosphorylated cholinesterase. For all three derivatives the k(+3)-pH plots are bell-shaped, with a pH optimum between 8.0 and 8.5. The changes in k(+3) above and below the optimum fit theoretical curves for the dissociation of groups of pK 6.9 and 9.8. 5. The relevance of these results to binding, acylation and deacylation of both inhibitors and substrates is discussed.
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PMID:Effect of pH on inhibition and spontaneous reactivation of acetylcholinesterase treated with esters of phosphorus acids and of carbamic acids. 607 Jan 26

A clinical and serological study was performed on 267 of 636 volunteers vaccinated against Argentine hemorrhagic fever with the XJCl3 attenuated strain of Junin virus seven to nine years earlier, in order to determine their long-term evolution. This study included a clinical examination, a chest roentgenogram, an electrocardiogram, and the following laboratory determinations: white and red cell count, number of platelets, hematocrit, hemoglobin, sedimentation rate (Katz index), urea, nitrogen, glucose concentration, cholesterol, GOT, GPT, gamma GT, alkaline phosphatase, cholinesterase, and total bilirubin. Neutralization reactions were performed to determine presistence of antibody levels. All clinical and laboratory findings were within normal limits, excluding a long-term pathology attributable to the virus. Of 165 tested sera, 153 (90.3%) had detectable levels of neutralizing antibodies, and the rest had no antibodies after this time. Although these people live in the endemic area, it is considered that only the 9% that had increased antibody levels had suffered a reinfection during the seven- to nine-year period, which acted as a booster. This figure aproximately coresponds to the subclinical infection value found in the region. In the rest, the persistence of antibodies is attributed to the immunization achieved with the vaccine employed.
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PMID:Immunogenicity of A/USSR (H1N1) subunit vaccine in unprimed young adults. 627 Feb 79

To determine the effects of low-dosage organophosphate administration on exercise in a hot environment, malathion (7.5 mg/day, 4 days) was administered IP to rats, and effected a 35% (p less than 0.01) reduction in plasma cholinesterase levels. Treadmill endurance (9.14 m/min, no incline, 35 degrees C ambient) was unaffected when the animals were exercised to hyperthermic exhaustion (Tre approximately 43 degrees C). While rates of heat gain were similar between groups, malathion-treated rats displayed higher Tsk (p less than 0.05) at a number of sampling times during the treadmill run. While creatine phosphokinase levels were unaffected by either cholinesterase inhibition or exercise in the heat, lactate dehydrogenase activities were increased (p less than 0.01) in both groups following hyperthermic exhaustion. Although plasma levels of lactate, potassium, urea nitrogen, and creatinine were all significantly (p less than 0.01) increased as a result of exercise in the heat, these increments were not exacerbated by cholinesterase inhibition. Results generally indicated that at this moderate level cholinesterase inhibition, malathion administration did not adversely affect physiological, physical, or thermoregulatory efficacy.
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PMID:Malathion administration: effects on physiological and physical performance in the heat. 665 21

Adult, male rats (300-325 g) were treated with pyridostigmine bromide (n = 22) or saline (n = 22) to quantitate the effects of cholinesterase inhibition (64%) on the ability to work (9.14 m/min, level treadmill) in the heat (35 degrees C). Pyridostigmine-treated rats had a mean endurance of 23 min, whereas saline-treated animals ran for nearly 35 min (P less than 0.001). Rates of rectal and skin temperature increments were significantly higher (P less than 0.001) in pyridostigmine-treated rats as were water losses (P less than 0.001). Exercise in the heat to hyperthermic exhaustion effected anticipated increments in circulating urea nitrogen, creatinine, lactate dehydrogenase, and potassium levels, whereas pyridostigmine pretreatment had additive effects on lactate and creatine kinase concentrations. Additionally, pyridostigmine elicited a significant (P less than 0.01) hyperglycemia before exercise, an effect noted also with other organophosphate simulants. We concluded that pyridostigmine-induced cholinesterase inhibition had a variety of debilitating effects during work in the heat.
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PMID:Effects of pyridostigmine on ability of rats to work in the heat. 672 66


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