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)

In experimental investigations on Eimeria stiedai infected rabbits, serum enzymatic studies have been carried out in correlation with the examination of parasitological and pathological parameters. The rabbits were orally infected with a single dose of either 100,000 or 250,000 sporulated oocysts. Increase of the activity of the sorbit dehydrogenase (SDH), glutamate oxalate transaminase (GOT), glutamate pyruvate transaminase (GPT) and glutamate dehydrogenase (GlDH) could be found first between 3 and 10 days after infection indicating the beginning of the acute phase of liver coccidiosis. The increase of the conjugated bilirubin and of the gamma-glutamyl-transferase (gamma-GT) could be found not earlier than 10 days after infection and is to be explained as sign of disturbed efficiency of excretion. The various investigated parameters reached their peak of alteration about the end of the prepatent period and at the beginning of patency between 14 and 21 days after infection. The results emphasize the value and usefulness of serum enzymes, particularly the glutamate dehydrogenase (GlDH) and the gamma-glutamyl-transferase (gamma-GT) with about 30fold activity, as indicators in the course of Eimeria stiedai infection of rabbits. The enzymes returned to physiological values at the end of the experiment, 42 days after infection. Significant differences could not be detected within the infected groups. The activities of the alkaline phosphatase (AP), leucine aminopeptidase (LAP), choline esterase (ChE), lactate dehydrogenase (LDH) and isoenzym 1 (alpha-HBDH) showed only slight alterations and proved to be no significant parameters for the pathophysiological evaluation of the liver coccidiosis.
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PMID:[Alteration of enzyme activities in serum of Eimeria stiedai infected rabbits (author's transl)]. 73 5

The intrathecal administration of pertussis toxin (PTX) not only blocks the antinociceptive effects of the muscarinic cholinergic receptor agonist oxotremorine administered systemically, but also produces a long-lasting thermal allodynia in mice. The purpose of the present studies was to determine both the antinociceptive effects in normal mice and the antiallodynic effects in PTX-treated mice of systemically administered muscarinic cholinergic receptor agonists and cholinesterase inhibitors. In normal mice, antinociceptive effects were tested using a 55 degrees C water-bath tail-flick test. In mice treated 7 days previously with PTX (0.3 microg i.t.), antiallodynic effects were tested using a 45 degrees C water-bath tail-flick test. The nonselective high-efficacy muscarinic agonists oxotremorine, H-TZTP (3-(1,2, 5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine oxalate), and methylthio[2.2.1], (exo (+)3-(3-methylthio-1,2, 5-thiadiazol-4-yl)-1-azabicyclo[2.2.1]heptane oxalate), as well as vedaclidine, a mixed M(2)/M(4) muscarinic receptor partial agonist and M(1)/M(3)/M(5) muscarinic receptor antagonist, the nonselective partial agonists RS86 and pilocarpine, and the cholinesterase inhibitors physostigmine and tacrine all produced dose-related antinociception. Oxotremorine, H-TZTP and methylthio[2.2.1] produced dose-related reversals of PTX-induced thermal allodynia whereas vedaclidine produced a partial reversal and RS86 and pilocarpine, as well as physostigmine and tacrine, failed to reverse the allodynia. The present results provide further evidence that decrements in PTX-sensitive G(i/o)-protein functioning may be involved in initiating and/or maintaining some persistent or neuropathic pain states. Moreover, the present results suggest that muscarinic receptor agonists such as vedaclidine may be useful in the treatment of persistent pain states that are due at least in part to dysfunction of inhibitory second messenger systems.
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PMID:Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice. 1097 34

The enzymatic degradation of cocaine in blood samples, even during transport to a forensic laboratory, is a common problem in toxicological analysis. This can be avoided by the use of blood-sampling devices such as gray-top Vacutainers containing the cholinesterase inhibitor sodium fluoride. In the present study, which included 147 authentic cases, blood samples were collected into two different tubes, one containing fluoride/oxalate and one without stabilizing agents. In all cases, both samples were analyzed for drugs of abuse using Abbott FPIA immunoassays after precipitation and gas chromatography-mass spectrometry (GC-MS) for quantitative analysis. The cannabinoid immunoassay showed markedly lower values in the fluoride-containing samples; this was investigated further and could be explained by hemolysis of these samples. In addition, the concentrations of 11-nor-delta9-tetrahydrocannabinol-9-carboxylic acid (THCCOOH) were lower in these samples. A stability study with the THCCOOH acyl glucuronide showed that it is unstable in unpreserved serum, which could explain our observation. GC-MS quantitative data for amphetamine and derivatives, opiates, delta9-tetrahydrocannabinol, and 11-hydroxy-delta9-tetrahydrocannabinol were essentially identical; however, they also differed substantially for cocaine, cocaethylene, ecgonine methylester, and benzoylecgonine. Unexpectedly, the concentrations of benzoylecgonine in unpreserved serum were almost half as high as in the fluoride-containing samples.
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PMID:Importance of vacutainer selection in forensic toxicological analysis of drugs of abuse. 1149 88

Donepezil, a cholinesterase inhibitor with good central nervous system penetration, has been crystallized as a tertiary amine salt with a disordered oxalate anion to give the title compound, (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidinium hydrogen oxalate trihydrate, C24H30NO3+.C2HO4-.3H2O. The indanone and piperidine ring planes are inclined at an angle of 33.4 (1) degrees. A comparison is made with the piperidinium cation bound in acetylcholinesterase in the solid state. The methylene units bridging the indanone-piperidine-benzyl groups determine the molecular shape and conformational features. The structure is stabilized mainly by O-H...O and N-H...O hydrogen bonds, with water molecules mediating interactions between oxalate anions and donepezilium cations.
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PMID:Donepezilium oxalate trihydrate, a therapeutic agent for Alzheimer's disease. 1714 11

Bizerine-oxalate of hexamethylene-bic-[N-methylcarbamic acid-3-(2-dimethylaminomethyl)pyridyl ether] exhibits the properties of acetylcholine esterase (AChE) inhibitor, being comparable in this respect in in vitro tests to aminostigmine. Bizerine is 2.5 and 6.7 times less active in these tests than proserine and distigmine, respectively, but it forms more stable complex with the enzyme. Bizerine is 10-80 times less toxic for laboratory mammals as compared to prozerine; it is 3-60 times more active on the isolated urinary bladder of rats, but it is 100-500 times less effective on the spinal muscle of leeches and skeletal muscles of mice and rats. Bizerine actively inhibits intestinal cholinesterase (ChE) of guinea pigs. In systematic use, it does not inhibit brain ChE of mice. Bizerine is a prolonged peripheral muscarinic potentiating inhibitor of ChE and activator of intestinal peristalsis.
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PMID:[Bizerine: new anticholinesterase drug with selective gastrointestinal action]. 2091 51

Objectives: Curcuma amada Roxb. (Mango ginger) was evaluated for anti-obesity, anti-amnesic and neuroprotection using high-fat and high-sugar diet (HFHS)-induced obesity and cognitive impairment in rats. Methods: Animals were exposed to HFHS diet to evaluate lipid parameters and subjected to Y maze test and Pole climbing test to evaluate the memory. In addition, oxidative stress parameters, acetyl cholinesterase activity (AChE), neurochemicals and histopathology were assessed in the brain. Results: HFHS diet led to increased body weight and lipid parameters (total cholesterol, low-density lipoprotein [LDL], and very low-density lipoprotein [VLDL], triglycerides [TG]) but not high-density lipoprotein (HDL). Elevated serum glutamate oxalate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT), oxidative biomarker, decreased enzymatic and non-enzymatic antioxidants, Acetylcholinesterase (AChE) activity and reduced percentage of spontaneous alternation behaviour (% SAB in Y-maze test) as well as reduced serotonin and dopamine levels and neurodegeneration were observed in HFHS diet-fed rats. Curcuma amada (CAAE1, 100 mg/kg and CAAE2, 300 mg/kg) treatment to HFHS diet-fed rats (21 days after HFHS diet feeding alone) showed dose-dependent activity and ameliorated the HFHS diet-induced alterations in lipid parameters related to obesity, hepatological parameters, memory, oxidative stress, neurochemicals and neurodegeneration. Furthermore, 300 mg/kg of C. amada (CAAE2) augmented the memory by inhibiting acetylcholinesterase (AChE) activity; it also ameliorated the effect of antioxidants such as glutathione, superoxide dismutase (SOD), and total thiol and mitigated the effect of malondialdehyde (MDA). CAAE2 also controlled the level of dopamine and serotonin and reduced the neurodegeneration in the hippocampus CA1 region. Discussion: The results of the present study indicated that treatment with C. amada 300 mg/kg (CAAE2) attenuated the HFHS diet-induced obesity, memory loss, oxidative stress, and neurodegeneration. These study results indicated that the administration of C. amada offers a potential treatment option for obesity and memory loss, and it requires further preclinical and clinical evaluations.
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PMID:Protective effect of Curcuma amada acetone extract against high-fat and high-sugar diet-induced obesity and memory impairment. 3114 94