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

---

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

The intracellular distribution of acetylcholinesterase (AChE) was determined in adult rat anterior gracilis muscles. Echothiophate iodide (ECHO), a water-soluble cholinesterase inhibitor, was applied to muscles in situ to eliminate extracellular and/or extracellularly oriented enzyme. Control and ECHO-treated muscles were either cut into 1-mm segments and assayed for AChE activity or cytochemically stained for AChE. Subsequent analysis by light and electron microscopy showed that the AChE stain inside myofibers was highly localized and clearly visible only in the zone immediately underlying the point of nerve-muscle contact. Biochemical assay of muscle segments showed intracellular AChE to be most highly concentrated in regions containing large numbers of endplates (approximately twice the activity of endplate-free areas). Since such "endplate-rich" segments are in fact mostly extra-synaptic tissue, we conclude that intracellular AChE of adult rat gracilis myofibers, although present along the length of the cell, is more than two times as concentrated in sub-synaptic areas as compared to extra-synaptic areas. This result must be carefully considered when attempting to identify "endplate-specific" AChE activity of mammalian muscle, and further points to the importance of neural influences on AChE metabolism/regulation.
...
PMID:Intracellular acetylcholinesterase of adult rat myofibers is more concentrated in endplate than non-endplate regions. 358 68

This paper alerts investigators to the possibility of an excessive early release from the Alzet osmotic pump. In this research, rats were implanted with 7-day minipumps (model 2001) containing 24 mg/kg/day pyridostigmine, and blood samples were taken at intervals from 5 to 60 min after implantation. All samples showed that blood serum cholinesterase activity was markedly depressed as compared with those of controls. This finding demonstrated that animals were receiving the drug well before the pump's 4- to 6-hr start-up transient period. In a separate study, dye filled pumps were monitored for release when dropped into distilled water at 24 degrees C or 37 degrees C. The pump in the 37 degrees C water released approximately 5% of its contents within 30 sec of submersion, while the pump in the 24 degrees C water released virtually no dye. The early release appears to have been caused by expansion of the pump's contents when the pump, at room temperature, was implanted in the warmer animal.
...
PMID:Premature excess release from the Alzet osmotic pump. 361 44

The time course of physostigmine (Phy), its metabolites and activity of cholinesterase (ChE) in plasma were studied after intravenous bolus administration of [3H]Phy (100 micrograms/kg) to beagle dogs. The maximal inhibition of ChE (78%) in plasma at 2 min correlated with the largest concentration of physostigmine (124 ng/ml). The concentration of physostigmine decreased by 88% to 16 ng/ml at 45 min when the activity of ChE was still 59% inhibited. Acetylcholinesterase activity in four regions of the brain (medulla, striatum, cerebellum and cortex) was not significantly different from controls at 70 +/- 5 min after administration of physostigmine. Concentrations of physostigmine and its metabolites determined by HPLC were not significantly different in different regions. In plasma, physostigmine was found, together with eseroline and two other metabolites M1 and M2. At 45 min, only 18% of total radioactivity was due to physostigmine and 52% was due to the major metabolite M1. On the contrary, in regions of the brain, metabolite M1 represented only 1.9-3.37% of total radioactivity at 70 +/- 5 min. Pharmacokinetic parameters, obtained in the dog, were compared to previously published data in rat and man. The elimination half-life (beta) was 30.7 min in the dog as compared to 15 min in rat and and 21.7 min in man. The Vd (ml/kg) was higher than total body water volume in all three species: dog (1832), rat (1352) and man (664), indicating sequestration of the drug in body compartments. Clearance (ml/min/kg) was found to be 41.2 in dog, which compares to 62 in rat and 22 in man.(ABSTRACT TRUNCATED AT 250 WORDS)
...
PMID:Pharmacokinetics and pharmacodynamics of physostigmine after intravenous administration in beagle dogs. 365 15

The effects of tertiary amine local anesthetics (procaine, mepivacaine, lidocaine, tetracaine, dibucaine, and bupivacaine) and chlorpromazine were investigated for rabbit muscle acetylcholinesterase and human serum cholinesterase. The muscle enzyme was poorly inhibited by local anesthetics containing an amide linkage. The serum cholinesterase was inhibited by all those compounds, their relative potencies being proportional to their octanol/water partition coefficients. The dissociation constants of tetracaine and procaine, ester anesthetics, were 1000-fold and 100-fold, respectively, that which would be expected from their partition coefficient basis respective to the other amide anesthetics. Procaine showed competitive inhibition of serum cholinesterase, whereas for most anesthetics a mixed type of inhibition was observed. Procaine probably binds at the main anionic site, while the other positively charged anesthetics bind to either the catalytic centre or to the peripheral or modulator anionic site, modifying the kinetic behaviour of cholinesterase as has been demonstrated by the appearance of negative cooperativity for binding to the substrate.
...
PMID:Inhibition of human serum and rabbit muscle cholinesterase by local anesthetics. 367 16

Adult male Long-Evans rats were intermittently exposed to 2450 MHz CW microwaves at an average power density of 0.5 mW/cm2 for 90 days. The resulting SAR was 0.14 W/kg (range 0.11 to 0.18 W/kg). The animals were exposed 7 h/day, 7 days/wk, for a total of 630 h in a monopole-above-ground radiation chamber while housed in Plexiglas holding cages. Daily measures of body mass and food and water intake indicated no statistically significant effects of microwave exposure. Monthly assessment of reactivity to electric footshock, levels of cholinesterase and sulfhydryl groups in blood, and 17-ketosteroids in urine revealed no reliable differences between 14 sham-exposed and 14 microwave-exposed rats. After the 90 days of exposure, seven rats, randomly chosen from each group, were assessed for open-field behavior, shuttlebox performance, and schedule-controlled (IRT schedule) lever pressing for food pellets. Statistically significant differences between microwave-exposed and sham-exposed rats were observed in shuttlebox performances and lever pressing. Post mortem measures of mass of several organs and microscopic examination of adrenal tissue revealed no differences between the two groups of animals.
...
PMID:Behavioral and physiological effects of chronic 2,450-MHz microwave irradiation of the rat at 0.5 mW/cm2. 373 1

We have recently reported that acute intraperitoneal administration of pyridostigmine bromide to rats resulted in significant decrements in physical performance in the heat, adverse thermoregulatory effects, and exacerbated elevations in several indices of heat/exercise injury. Since it will be consumed orally as a prophylaxis for organophosphate poisoning, pyridostigmine was dissolved in the drinking water of rats. Consumption of pyridostigmine for 7 days (n = 34, 6.6 mg/day) resulted in a 23% (p less than 0.001) reduction of circulating cholinesterase when compared with a control group (n = 31) while ingestion for 14 days (n = 35, 8.9 mg/day) elicited a 39% (p less than 0.001) inhibition of circulating cholinesterase when compared to a second control group (n = 33). Water and food consumption, rate of weight gain, and overt behavior were unaffected by pyridostigmine consumption. When approximately half the animals in each group were exercised (9.14 m/min) in the heat (35 degrees C) to hyperthermic exhaustion (Tre = 42.5-43 degrees C, rats unable to right themselves), pyridostigmine consumption for 14 days effected a significantly (p less than 0.05) increased rate of weight loss, but no further effects on thermoregulation or performance were noted. Several minor increments were observed in clinical indices of heat/exercise injury in rats consuming pyridostigmine for 14 days. These data indicate that oral dosages of pyridostigmine can probably be titrated to levels of cholinesterase inhibition which are efficacious in prophylaxis against organophosphate toxicity without significant effects on selected physiologic and metabolic processes.
...
PMID:Oral pyridostigmine administration in rats: effects on thermoregulation, clinical chemistry, and performance in the heat. 378 59

L. W. Haynes and M. E. Smith have reported [(1985) Biochem. Soc. Trans. 13, 174-175] that glycyl-L-glutamine (Gly-Gln) increases the A12 and G4 forms of acetylcholinesterase (AcChoEase) in cultured embryonic rat skeletal muscle. Since Gly-Gln meets the criteria established for the neurotrophic factor (NF) in extracts of central nervous system/sciatic nerves that maintains AcChoEase and butyrylcholinesterase (BtChoEase) in the denervated cat superior cervical ganglion (SCG) in vivo, it was tested by the latter procedure. Solutions of Gly-Gln (10(-7)-10(-3) M) in 0.9% NaCl solution were infused for 24 hr via the right common carotid artery of cats with preganglionically denervated SCG, following ligation of the external carotid and lingual arteries. At 48 hr postdenervation, the AcChoEase and BtChoEase contents of the right SCG were within the range of similarly treated controls infused with 0.9% NaCl solution; the AcChoEase and BtChoEase contents of the left SCG, where the infused solutions arrived by way of a much more circuitous route, were significantly elevated at concentrations of Gly-Gln of 10(-5) M and higher. This suggested that the neurotrophic effect on the left SCG was produced by a metabolite of Gly-Gln. Accordingly, glycine, L-glutamine, and glycyl-L-glutamic acid (Gly-Glu) were then tested. Glycine and L-glutamine were inactive; Gly-Glu, 10(-6)-10(-5) M, exerted a significantly positive neurotrophic effect at both the right and left SCG; at 10(-4) M, the effect was absent. The method employed currently for preparation of extracts of SCG for assay of AcChoEase, BtChoEase, and protein contents (homogenization of scissor-minced ganglia in water) was compared with homogenization in molar NaCl/1% Triton X-100. Values obtained by the former procedure, in comparison with the latter, were 91% +/- 7% for AcChoEase and 83% +/- 7% for BtChoEase, expressed as substrate hydrolyzed per mg of protein per min.
...
PMID:Glycyl-L-glutamine, a precursor, and glycyl-L-glutamic acid, a neurotrophic factor for maintenance of acetylcholinesterase and butyrylcholinesterase in the preganglionically denervated superior cervical ganglion of the cat in vivo. 386 Aug 56

Captopril (50 mg orally) produced a significant fall in systolic and diastolic blood pressure in six normotensive sodium replete subjects, without a rise in heart rate. On captopril, there was no change in the expected normal increase in heart rate on standing. Supine plasma noradrenaline was not reduced by captopril and normal postural increases were maintained. Atropine (0.04 mg/kg i.v.) reduced the difference in blood pressure change between captopril and placebo. Facial immersion in water produced a bradycardia. This change was abolished by atropine and attenuated both by captopril and edrophonium (10 mg i.v.), a cholinesterase inhibitor. Lying down after 6 min standing produced an immediate transient tachycardia, which was abolished by atropine and attenuated by captopril. Blood pressure and heart rate rose after a cold pressor test on both captopril and placebo. The tachycardia during the Valsalva manoeuvre was inhibited by edrophonium and to a lesser extent by captopril. The effects of captopril and edrophonium were additive. Parasympathetic activity of captopril may contribute to its haemodynamic profile.
...
PMID:Evidence of parasympathetic activity of the angiotensin converting enzyme inhibitor, captopril, in normotensive man. 388 May 23

In the substantia nigra, acetylcholinesterase may have a non-cholinergic function. Previous work suggests that release of acetylcholinesterase locally in the substantia nigra leads to a net increase in dopaminergic activity in the ipsilateral striatum. To investigate this hypothesis, acetylcholinesterase was microinjected bilaterally into the substantiae nigrae of awake rats and stereotyped behaviour used as an indication of increased dopaminergic activity in the striatum. Acetylcholinesterase increased stereotypy in rats, while butyrylcholinesterase and the vehicle, distilled water, were ineffective. The functional significance of acetylcholinesterase in the substantiae nigrae of freely moving animals is discussed in the light of its apparent association with dopaminergic rather than cholinergic systems.
...
PMID:Application of acetylcholinesterase to the substantia nigra induces stereotypy in rats. 391 82

The effect of hypoparathyroidism and low blood calcium on enzyme levels in rat liver and kidney is shown. Four animal groups were used: parathyroidectomized (PTX), PTX with CaCl2 added in the drinking water, sham-operated controls and sham-operated with CaCl2 added in the drinking water. PTX significantly lowered serum parathyroid hormone (PTH) and calcium. Supplementation of CaCl2 in the drinking water increased serum Ca levels in PTX rats but not in the controls. Significant changes in several liver and kidney enzymes were seen. Most affected were the liver NADP dependent enzymes, glucose-6-phosphate dehydrogenase and malic enzyme. Similar patterns but with relatively smaller changes were seen in the liver enzymes, lactic dehydrogenase, hexokinase, and aspartate transferase. No significant differences between the groups were seen in the levels of malic dehydrogenase, isocitric dehydrogenase, fructose-6-phosphate kinase and cholinesterase. In the kidney, which was less affected than the liver, the only significant difference was seen in the level of malic enzyme. Serum total lipids in the PTX group were significantly lower. All the changes seen were partially reversed by Ca supplementation in the drinking water.
...
PMID:Biochemical change in the liver and kidney of rats following parathyroidectomy. 400 1


<< Previous 1 2 3 4 5 6 7 8 9 10 Next >>

---