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)

Treatment of rats with aurantine for 7-30 days reduces the growth and development of animals, and especially of skeletal muscles. Low relative weight of muscles in aurantine-treated animals was accompanied by low resting and action membrane potentials. Incorporation of labelled uridine and lysine into muscles, heart, brain and liver was decreased. Retardation in the growth and development of skeletal muscles resulted into unfavourable shift of the ratio body weight/surface and led to prevalence of catabolic processes over anabolic ones (increased oxygen consumption, heart and respiration rate in experimental animals). These changes are probably related not only to the inhibition of protein synthesis, but to disturbance of regulatory mechanisms, which reveals itself in an increased norepinephrine content of the brain stem and in the increased cholinesterase activity in cardiac pacemaker.
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PMID:[Retardation of growth and development of rats induced by inhibition of protein synthesis at early postnatal ontogenesis]. 5 9

The use of atropine to block the effects of acetylcholine and pralidoxime chloride to restore cholinesterase in the blood, along with supportative therapy, intravenous fluids, and oxygen, prevented death in five cases of intentional ingestion of 25% diazinon. Treatment of such cases must be tailored to the condition of the patient, and all residual poison in the stomach must be removed as rapidly as possible with gastric lavage to prevent absorption of the poison.
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PMID:Five cases of intentional ingestion of 25 percent diazinon with treatment and recovery. 65 58

As a continuation of our efforts to develop and study inhibitors which act presynaptically on neuromuscular function, sulfur analogues of hemicholinium-3 (HC-3, 1) and acetyl-seco-hemicholinium-3 (AcHC-3, 3) were prepared. In each case sulfur is substituted for the noncarbonyl oxygen in HC-3 (1) and AcHC-3 (3). As expected on the basis of conformational differences between acetylcholine and acetylthiocholine both of the thio analogues are produced in the seco form and do not cyclize spontaneously or when subjected to aqueous, acidic conditions up to 100 degrees C. Both compounds are stable in aqueous pH 7.4 solutions at 37 degrees C and in slightly acidic D2O solutions for more than 24 h. While thio-seco-hemicholinium 3 (11) is stable in the presence of acetylcholinesterase and butyrylcholinesterase in H2O at pH 7.4, acetylthio-seco-hemicholinium-3 (12) reacts within seconds to form the hemiacetal form of thiohemicholinium-3 (16). Mouse toxicity studies (LD50) indicate that while 12 is approximately as toxic as HC-3 (1) and AcHC-3 (3), 11 is 226 times less toxic. As in the studies with 1 and 3, mice were protected from 11 by choline and slightly by neostigmine. It is of interest, however, that almost equal and intermediate protection against 12 was afforded by choline and neostigmine. Structure-toxicity relationships of 1,3,11, 12, and 16 are discussed.
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PMID:Effect of sulfur substitution for the noncarbonyl oxygen in hemicholinium-3 and acetyl-seco-hemicholinium-3. Synthesis, biological activity, and structure-toxicity relationships. 83 27

Release of peroxidase from secretory cells of rat lacrimal gland upon cholinergic stimulation was studied in vitro with single lobules and isolated cells (lacrimocytes). Isolated lobules, kept in Eagle's medium, remain structurally intact and reaction product of peroxidase is confined to cisternae of rough endoplasmic reticulum, elements of the Golgi apparatus, and all secretory granules. Morphologically, exocytosis occurs by membrane fusion and discharge of granule content. The highest rate of peroxidase released from lobules is observed at 10(-4) M carbamylcholine. The specific activity of peroxidase released into the medium is fourfold higher as compared to the lobules. Release of peroxidase is suppressed by atropine when added before or after the addition of carbamylcholine. At 4 degrees C, no peroxidase release occurs upon cholinergic stimulation. The exocytotic release of peroxidase is dependent on energy supply, as indicated by substantial inhibition (at 37 degrees C) under anoxic conditions or in the presence of dinitrophenol, KCN, or carboxyatractyloside. Furthermore, the process is sensitive to colchicine and vinblastine. Isolated lacrimocytes, consiting of 95% secretory acinar cells, are prepared by digestion with collagenase, hyaluronidase, and trypsin. They retain the characteristic polarity of secretory cells in situ, and localization of peroxidase is the same as in lobules. Since isolated lacrimocytes respond to cholinergic stimulation in the same way as lobules, the receptors are not damaged by the isolation procedure and appear to be associated directly with the exocrine cell. Oxygen uptake by isolated lacrimocytes is about 14 nmol O2 X min-1 X 10(-6) cells; it is about doubled by uncoupling with dinitrophenol. Oxygen uptake rises by 20-30% above the resting rate upon cholinergic stimulation. This additional uptake is suppressed by atropine or by added cholinesterase, indicating that continuous receptor occupancy may be required for the energy demand by exocytosis. On the basis of the specific activity of peroxidase in the medium, the energy demand resulting from cholinergic stimulation is estimated to be 0.08 mumol ATP (or energy-rich phosphate bonds) per microgram of protein released from the lacrimocytes.
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PMID:Exocytosis in secretory cells of rat lacrimal gland. Peroxidase release from lobules and isolated cells upon cholinergic stimulation. 95 71

The action of the cholinesterase reactivator isonitrosine on gas homeostasis was studied in experiments on intact dogs. It has been found that oxygen consumption and CO2 release by tissues were enhanced within the period from 15 min to 6 days following isonitrosine administration. Simultaneously, oxygen return by the blood was improved. Such action of isonitrosine was unrelated to its effect on the cholinesterase activity of red blood cells.
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PMID:[The effect of isonitrozine on gas homeostasis]. 145 58

Seventy-one male and 52 female F 344 rats with leukemia used as controls in the 30-month inhalation studies were characterized by hematological and clinico-biochemical findings. Hematological findings revealed that the leukocyte count, mean corpuscular volume, and mean corpuscular hemoglobin increased in both sexes of leukemic rats showing profound anemia, while the platelet count, erythrocyte count, hematocrit, and hemoglobin concentration decreased. In these rats, the serum levels of low density lipoprotein, free cholesterol, total bilirubin, blood urea nitrogen, and triglyceride and the activities of glutamic oxalacetic transaminase, glutamic pyruvic transaminase, creatine phosphokinase, alkaline phosphatase, and lactate dehydrogenase increased markedly and the level of high density lipoprotein, the oxygen partial pressure, and the cholinesterase activity decreased. Clinical signs such as decrease in redness of the eyes, decrease in body weight, abdominal distension, staining of the public region, and debility were seen in most leukemic animals. These clinical signs and hematological and clinico-biochemical findings may be helpful in diagnosis of leukemia in long-term experiments.
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PMID:Hematological and clinico-biochemical characteristics of leukemia in Fischer 344 rats. 150 22

Succinylcholine is a depolarizing neuromuscular blocking drug, which is rapidly hydrolyzed by the enzyme pseudocholinesterase. In Greyhounds, the metabolism of certain drugs is atypical relative to other breeds, and it has been suggested that Greyhounds may be an atypical population, with lower pseudocholinesterase activity, slower hydrolysis of the drug succinylcholine, and a prolonged duration of action of the drug, compared with a mixed-breed control population. Six healthy adult Greyhounds and 6 healthy adult mixed-breed dogs were studied. Blood was drawn from each dog and analyzed for serum cholinesterase activity, and a biochemical profile was done to verify normal liver function. The dogs were anesthetized with methohexital (10 mg/kg) and isoflurane (1.25 minimal alveolar concentration) in 100% oxygen. Ventilation was controlled, fluids were administered IV (lactated Ringer solution, 10 ml/kg/h), and blood gases, blood pressure, and heart rate were monitored. The right hind limb was immobilized and a force transducer was used to monitor twitch strength of the interosseous muscle with supramaximal stimulation of the tibial nerve. Succinylcholine was administered to each dog 3 times at a dosage of 0.3 mg/kg. After drug administration, the time to 50% recovery of twitch strength (single twitch, 1/s), and 50% recovery of train-of-4 was determined. Subsequent doses were administered after complete recovery. The time to 50% recovery after succinylcholine administration in Greyhounds (38 minutes, dose 1, single twitch) was not significantly different than the time to 50% recovery in mixed-breed dogs (29 minutes, dose 1, single twitch), using either monitoring technique. Pseudocholinesterase activity was also not significantly different between the Greyhounds (1,685 mU/ml) and the mixed-breed dogs (1,588 mU/ml).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacodynamic properties of succinylcholine in greyhounds. 188 92

Preliminary disposition studies of the investigational, long-acting muscle relaxant doxacurium chloride (Nuromax) have demonstrated dual elimination by renal and hepatobiliary pathways, as well as slow hydrolysis by plasma cholinesterase. The present study compares the kinetics and dynamics of doxacurium in eight ASA physical status I or II elderly patients (67-72 yr of age) and eight ASA I or II young patients (22-49 yr of age). After institutionally approved written informed consent, kinetic and dynamic measurements were made after a 25-micrograms/kg bolus injection of doxacurium during 1.25 MAC nitrous oxide/oxygen/isoflurane anesthesia. Maximum twitch depression was similar in older patients (96.4% +/- 1.3%) to that in the young patients (96.6% +/- 1.8%). The time to achieve this level of block was significantly longer in the elderly than in the young (11.2 +/- 1.1 min versus 7.7 +/- 1.0 min, respectively). Recovery times to twitch heights of 5% and 25% of control tended to be prolonged and were more variable in the elderly (82.6 +/- 17.2 and 97.1 +/- 20.1 min, respectively) than in the young (54.8 +/- 9 and 67.5 +/- 8.2 min, respectively). Elimination half-life (96 +/- 20 min) and clearance (2.47 +/- 0.69 mL.kg-1.min-1) in the elderly patients were not statistically different from values found in the younger group. Volume of distribution at steady state in the elderly (220 +/- 80.2 mL/kg) was significantly larger than in the young (150 +/- 40.0 mL/kg).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetics and pharmacodynamics of doxacurium in young and elderly patients during isoflurane anesthesia. 214 83

The biochemical changes of the elements of cholinergic neurotransmission (choline acetyltransferase, ChAT; acetylcholinesterase, AChE; butyrylcholinesterase, BuChE; and muscarinic cholinergic receptors, mAChR) as well as the electrolyte content were studied in ischemic lumbar spinal cord segments of newborn pigs. Ischemia was elicited by ligating the aorta for 30 min. Although no significant changes were observed in the sodium, potassium and calcium content of ischemic spinal cords, the calcium content was slightly elevated, to 119.3% of the control value. Whereas significant depletions were observed in both AChE and ChAT activities (to 69.1 and 87.7% of the control value, respectively), there was no significant change in BuChE activity as compared to the control value. The mAChR were also decreased, from 33.25 +/- 2.2 to 27.18 +/- 1.9 fmol/mg protein, while the Kd value was not significantly altered. It is concluded that even a relatively brief interruption of the oxygen supply can cause severe damage in the lumbar spinal cord of the newborn pig, affecting the cholinergic neurotransmission elements. This animal model might be suitable for studying the effects of hypoxia in newborns and children during chest operations involving the descending aorta.
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PMID:Effects of ischemia on cholinergic neurotransmission and electrolyte content in newborn pig lumbar spinal cord. 215 20

Bambuterol (the bisdimethylcarbamate prodrug of terbutaline) is a new bronchodilator with a prolonged duration of action due to its inhibition of plasma cholinesterase during metabolism. The effect of bambuterol on suxamethonium-induced neuromuscular blockade was studied in 10 patients undergoing elective laparotomy. Thirty mg of bambuterol was given 2 h before anaesthesia, which was performed with thiopentone, fentanyl, halothane and nitrous oxide in oxygen. Neuromuscular function was monitored using supramaximal train-of-four stimulation of the ulnar nerve and a force displacement transducer. Suxamethonium 1 mg.kg-1 was given i.v. for endotracheal intubation. Plasma cholinesterase activity was measured before and after intake of bambuterol and during anaesthesia. The results from the 10 patients were compared with those of 41 patients not given bambuterol but otherwise studied during the same conditions. Following bambuterol, all patients had a significant decrease of plasma cholinesterase activity (P less than 0.001) and the suxamethonium-induced blockade was 3-4 times prolonged compared to patients not given bambuterol (P less than 0.001). Five patients with very low plasma cholinesterase activity developed a long-lasting phase II block.
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PMID:The effect of bambuterol (carbamylated terbutaline) on plasma cholinesterase activity and suxamethonium-induced neuromuscular blockade in genotypically normal patients. 224 49


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