Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Pancuronium causes a powerful and highly selective inhibition of human serum cholinesterase in vitro. The inhibition was studied in serum from 14 individuals of both sexes (5-60 years of age) with normal reactions to suxamethonium. Pancuronium, in a concentration of 2.3 x 10(-7) M, caused a 50% inhibition of the enzymatic hydrolysis of acetylcholine, when this substrate was present in a concentration of 10 x 10(-3) M. The same I50 value was also found for a commercial preparation of human serum cholinesterase. The inhibition was reversible and competitive in type. Pancuronium inhibition of the acetylcholinesterase in human red blood cells and from the electric eel was more than one thousand times weaker. Thus pancuronium is one of the most selective inhibitors of serum cholinesterase described so far. The in vivo activity of the serum cholinesterase in four patients receiving pancuronium 0.1 mg/kg decreased, during the first 3 min, by 60-80%, from the pre-induction value. After this a slow recovery occurred with 40% depression remaining at 45 min after the injection. The tachycardia produced by pancuronium may be related to this selective inhibition of serum cholinesterase. It is suggested that relaxants which selectively inhibit serum cholinesterase also selectively block the cardiac muscarinic receptors.
Br J Anaesth 1975 Sep
PMID:The inhibition of cholinesterases by pancuronium. 119 83

Following 25 mug/day synthetic alpha-MSH administration, the liver regeneration of partially hepatectomized rats proved to be increased. The hormone treatment resulted in an enhanced alanine incorporation of the liver proteins, but this effect was uncertain on partially hepatectomized rats. Due to the hormone treatment the low liver protein content of the operated rats became normal. The pseudocholinesterase activity of the liver homogenate of alpha-MSH treated rats was also elevated. On the basis of these experiments authors are supposing some protein synthesis increasing effect of synthetic alpha-MSH.
Endokrinologie 1975 Sep
PMID:The effect of alpha-melanophor-stimulating hormone on liver regeneration and incorporation of amino acid in rats' liver protein. 122 18

1 Administration of corticosterone caused a 47% reduction in the cholinesterase (ChE) activity of homogenates of the rat anococcygeus muscle. 2 ChE activity was also reduced by morphine withdrawal and this effect was abolished by the corticosteroid synthesis inhibitor, metyrapone. 3 A single dose of reserpine reduced ChE activity in normal but not in adrenalectomized rats. 4 ChE activity was increased by adrenalectomy or by metyrapone treatment. 5 The mechanism of the corticosteroid-induced reduction in ChE activity is discussed. 6 The reduction in ChE activity produced by corticosterone, morphine withdrawal, or a single dose of reserpine might explain the leftward shift of the dose-% response curve to acetylcholine produced by these procedures in the isolated anococcygeus muscle of the rat.
Br J Pharmacol 1975 Sep
PMID:Reduction in the cholinesterase activity of the rat anococcygeus muscle produced by corticosterone. 123 31

Thirty-five patients with primary rhegmatogenous retinal detachments were followed for at least 6 months after scleral buckling procedures with subretinal fluid (SRF) drainage, in order to define factors influencing anatomic and visual outcome. Thirty-two cases were surgically reattached; three were not. Among the reattached cases, final visual acuity was poorer in patients with: older age; longer standing, more extensive detachments; detachment of the macula (with or without the development of a visible macular lesion); macular lesions; and higher SRF butyrylcholinesterase activity. These factors were themselves interrelated. Follow-up duration was only weakly related to final acuity, probably because of the long post-surgical follow-up. Phakic/aphakic status bore little relationship to final acuity. The type or timing relative to drainage of inflammation producing treatment was not related to final acuity.
Acta Ophthalmol (Copenh) 1975 Sep
PMID:Prognosis of primary rhegmatogenous retinal detachments. 1. Associations between clinical detachment characteristics, subretinal fluid butyrylcholinesterase and visual outcome following scleral buckling procedures. 124 87

76 cases of counterattack induced by acute organic phosphorus pesticides intoxication were analysed. The activity of cholinesterase did not show a significant difference before the counterattack as compared to that after the counterattack (P > 0.05). The average dosage of atropine for pre-atropinization was 58.6 +/- 2.7 mg/h and it was 203.9 +/- 17.7 mg/h between the post-counterattack and the second atropinization (P < 0.01). Compared the mortality in reaching and non-reaching the second atropinization was 22.8% VS 100% (P < 0.01). The survival rate was 37.5% in collaborating blood transfusion cases and 20.6% in noncollaborating ones (P > 0.05). We also studied on the treatment, mechanism, precursory symptoms, causes of death, degrees of intoxication and pesticide types etc.
Zhonghua Nei Ke Za Zhi 1992 Sep
PMID:[Clinical study of 76 cases of counterattack induced by acute organic phosphorus pesticides intoxication]. 130 44

In studies in developing countries, closed systems for mechanically mixing and loading hazardous pesticides have been shown to reduce exposure to workers. To evaluate the efficacy of closed systems in preventing worker exposure in the developing world, a cross sectional study was conducted at rural crop dusting airports in the cotton growing region of Nicaragua. Worker exposure was evaluated by measuring the activity of erythrocyte cholinesterase in the field with a new design battery operated colorimeter. The 10 mixer loaders at four airstrips with closed systems were compared with the 16 mixer loaders at four airstrips where pesticides were hand poured. Paradoxically, cholinesterase activity was 1.1 IU/ml blood (95% Cl 0.49-1.8) lower (inhibited) among workers in airstrips with closed systems than among workers hand pouring insecticides, after adjusting for weight of organophosphates sprayed in the past 14 days, and for prior training in safe use of pesticides. Mixer loaders with prior training had cholinesterase activity 0.83 IU (95% Cl 0.30-1.4) higher than untrained workers, and the weight of organophosphates sprayed was also a statistically significant predictor in the model. Unfortunately, management viewed the closed systems primarily as a production tool, rather than as a way to protect workers. Airstrips with closed systems were able to apply an average of 3250 lb organophosphates per worker in the 14 days before the survey compared with 849 lb per worker in airstrips without closed systems. Only three of 10 mixer-loaders at airstrips with closed systems had received formal training in safer use of pesticides. Because of shortage of personnel and transport, it was difficult for the responsible government agencies to train workers adequately and to enforce pesticide health and safety standards at multiple dispersed worksites.
Br J Ind Med 1992 Sep
PMID:Hazards of closed pesticide mixing and loading systems: the paradox of protective technology in the Third World. 139 Feb 66

A biomonitoring protocol, using blood cholinesterase (ChE) activity in livestock as a monitor of potential organophosphate nerve agent exposure during the planned destruction of US unitary chemical warfare agent stockpiles, is described. The experimental design included analysis of blood ChE activity in individual healthy sheep, horses, and dairy and beef cattle during a 10- to 12-month period. Castrated and sexually intact males, pregnant and lactating females, and adult and immature animals were examined through at least one reproductive cycle. The same animals were used throughout the period of observation and were not exposed to ChE-inhibiting organophosphate or carbamate compounds. A framework for an effective biomonitoring protocol within a monitoring area includes establishing individual baseline blood ChE activity for a sentinel group of 6 animals on the bases of blood samples collected over a 6-month period, monthly collection of blood samples for ChE-activity determination during monitoring, and selection of adult animals as sentinels. Exposure to ChE-inhibiting compounds would be suspected when all blood ChE activity of all animals within the sentinel group are decreased greater than 20% from their own baseline value. Sentinel species selection is primarily a logistical and operational concern; however, sheep appear to be the species of choice because within-individual baseline ChE activity and among age and gender group ChE activity in sheep had the least variability, compared with data from other species. This protocol provides an effective and efficient means for detecting abnormal depressions in blood ChE activity in livestock and can serve as a valuable indicator of the extent of actual plume movement and/or deposition in the event of organophosphate nerve agent release.
J Am Vet Med Assoc 1992 Sep 01
PMID:Characterizing biological variability in livestock blood cholinesterase activity for biomonitoring organophosphate nerve agent exposure. 139 73

In a prospective study we compared the usefulness of various laboratory tests (albumin, alpha-1-proteinase inhibitor (A1PI), cholinesterase (CHE), C-reactive protein, erythrocyte sedimentation rate, hematocrit) and activity indices (CDAI, VHAI) in relation to the disease activity by endoscopic criteria. Except for hematocrit highly significant differences (p less than 0.0005) of the mean values of all test results were found for patients without or with slight mucosal lesions compared with patients with severe inflammation of the mucosa. Further analysis of the data indicates the highest test efficiency (84%), sensitivity (80%), and specificity (88.6%) for CHE. CHE showed good correlations to all other tests; the highest correlation was found between CHE and VHAI (r = -0.78). We suggest that a suppression of CHE synthesis mediated by endotoxins and cytokines rather than an increased intestinal loss explains the decreased CHE in severe Crohn's disease. It is concluded from the data that CHE is a useful test to assess the inflammatory activity of Crohn's disease.
Scand J Gastroenterol 1992 Sep
PMID:Evaluation of different laboratory tests and activity indices reflecting the inflammatory activity of Crohn's disease. 141 Dec 85

The administration of 2-pyridine aldoxime methyl chloride (2-PAM Cl) is a standard part of the regimen for treatment of human overexposure to many organophosphorus pesticides and nerve agents. However, some literature references indicate that poisoning by carbaryl (1-naphthyl N-methyl carbamate), an insecticide in everyday use, is aggravated by the administration of 2-PAM Cl. This effect has been reported in the mouse, rat, dog and man. We have found that the inhibition of both eel acetylcholinesterase (eel AChE, EC 3.1.1.7) and human serum cholinesterase (human BuChE, EC 3.1.1.8) by carbaryl was enhanced by several oximes. Based on 95% confidence limits the rank order of potentiation with eel AChE was TMB-4 = Toxogonin > HS-6 = HI-6 > 2-PAM Cl. By the same criterion, the rank order of potentiation with human BuChE was TMB-4 > Toxogonin > HS-6 = 2-PAM Cl. Carbaryl-challenged mice also reflected a potentiation since TMB-4 exacerbated the toxicity more than 2-PAM Cl. Our hypothesis is that certain oximes act as allosteric effectors of cholinesterases in carbaryl poisoning, resulting in enhanced inhibition rates and potentiation of carbaryl toxicity.
Toxicol Lett 1992 Sep
PMID:Studies of the amplification of carbaryl toxicity by various oximes. 141 99

Acetyl- and butyrylcholinesterase (ACHE, BCHE) from evolutionarily distant species display a high degree of primary sequence homology and have biochemically similar catalytic properties, yet they differ in substrate specificity and affinity for various inhibitors. The biochemical information derived from analyses of ACHE and BCHE from human, Torpedo, mouse, and Drosophila, as well as that from the recombinant forms of their natural variants and site-directed mutants, can currently be re-examined in view of the recent X-ray crystallography data revealing the three-dimensional structure of Torpedo ACHE. The picture that emerges deepens the insight into the biochemical basis for choline ester catalysis and the complex mechanism of interaction between cholinesterases and their numerous ligands.
Trends Biochem Sci 1992 Sep
PMID:Excavations into the active-site gorge of cholinesterases. 141 13


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