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)

Five angusticeps-type toxins, F7, F8 and C10S2C2 from Dendroaspis angusticeps and C and FS2 from D. polylepis polylepis, were tested for action on the chick biventer cervicis nerve-muscle, the frog rectus abdominis muscle and the mouse phrenic nerve-diaphragm preparations. In the chick muscle, none of these toxins exhibited any stimulatory effect up to 100 micrograms/ml. In the frog muscle, the response to acetylcholine, but not to carbachol, was enhanced dose dependently by F7 and C. No appreciable effect was observed with the other three toxins. In the mouse diaphragm, also only F7 and C augmented responses to indirect stimulation and produced spontaneous fasciculations. On tetanic stimulation, a marked Wedensky inhibition was observed. Their stimulatory effect was abolished by d-tubocurarine. In the presence of d-tubocurarine as well as in the denervated mouse diaphragm, neither toxin increased responses to direct stimulation. In low-calcium (0.6 mM) or high magnesium (4.2 mM) medium, the stimulatory effect of both toxins was markedly attenuated. The resting membrane potential of the mouse diaphragm was not changed. The amplitude and frequency of MEPPs and the quantal content and the half-decay time of EPPs was increased. Both toxins also produced a stimulatory effect on the isolated guinea-pig ileum, which was abolished by atropine. In the rat atrial preparation, both toxins caused negative inotropic and chronotropic effects, which were reversed by atropine. If pretreated with atropine, these effects were completely prevented. Both F7 and C markedly inhibited the cholinesterase activity of the homogenized mouse diaphragm and frog rectus abdominis muscle but not that of the chick biventer cervicis muscle.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacological study on angusticeps-type toxins from mamba snake venoms. 315 33

Metoclopramide and ranitidine (10(-6)-10(-4) M) enhanced the electrical field stimulation-evoked contractions of isolated rat fundus and increased the gastric emptying in conscious rats. The enhancement of the fundus contractions by metoclopramide and ranitidine was abolished by atropine, but not by yohimbine, hexamethonium, propranolol or methysergide. The electrical field stimulation-evoked [3H]outflow from rat fundus strips, which has been preincubated with [3H]choline, was reduced by tetrodotoxin (10(-6) M) or in calcium-free medium, and potentiated by 4-amino-pyridine (3 X 10(-4) M), an acetylcholine (ACh)-releasing agent. Metoclopramide and ranitidine (10(-6)-10(-4) M) did not increase the [3H]outflow from the strips, in spite of causing a significant enhancement of their contractile response. However, both agents caused an increase in the ratio of [3H]acetylcholine/[3H]choline released into the superfusate during electrical field-stimulation. In rat fundus homogenates, metoclopramide and ranitidine showed a significant cholinesterase inhibition. These results seem to cast a doubt on the generally held ACh release hypothesis for the action mechanism of metoclopramide on one hand, and suggest, on the other hand, that cholinesterase inhibition contributes to some extent to the gastrokinetic effects of metoclopramide and ranitidine.
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PMID:Effect of metoclopramide and ranitidine on acetylcholine release from isolated rat stomach. 324 40

1. Using the theory of noise analysis an attempt was made to measure frequency and amplitude of miniature end-plate potentials (MEPPs) under conditions of vigorous transmitter release. Frog sartorius muscles were incubated in a depolarizing (32 mM-K+) medium which lacked Ca2+ to prevent transmitter release. Subsequently, when the membrane potential had become stable at about -40 mV, end-plates were superfused with 4 mM-Ca2+-containing medium for 1 min periods with 5 min intervals between the superfusions. 2. Most junctions ('fast' type) responded to Ca2+ with a relatively large, noisy depolarization (5.8-14.5 mV) which subsided rapidly during subsequent challenges with Ca2+. Other junctions ('slow' type) responded with only 1-1.6 mV depolarizations which were rather well sustained during the consecutive Ca2+ applications. 3. From the variance, E2, and the depolarization, V, caused by Ca2+ the frequency n and amplitude factor q of the MEPPs were calculated. Values of n were 3-4 x 10(4) and 0.1-1 x 10(4) s-1 in the fast- and slow-type junctions, respectively. The mean value of q was 0.16 mV; it remained more or less constant in the fast-type junctions, but tended to decline in the slow-type junctions. 4. As expected, cholinesterase inhibitors potentiated V and E2 as well as individual MEPPs. However, no advantage could be taken from this finding, since these drugs caused burst-like peaks superimposed on the voltage signal, precluding application of noise analysis. 5. The results strongly suggest that, at least in the fast-type junctions, K+ caused an extremely rapid depletion of the store of transmitter quanta, whose mean size did not change appreciably in the course of the experiment. However, in the slow-type junctions during prolonged incubation, it cannot be excluded that the gradual decline of q was due to the release of newly formed, unripe quanta.
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PMID:Analysis of quantal acetylcholine noise at end-plates of frog muscle during rapid transmitter secretion. 326 54

Elevation of extracellular potassium concentration ([K+]o) in cutaneous pectoris neuromuscular junction from 2 to 20 mM slowly increased the variability of the amplitudes of miniature end-plate currents (AMEPC-s), (coefficient of variation of AMEPC-s increased by 73%). Mean AMEPC-s, however, decreased but not markedly (by 14%). Comparable MEPC changes were observed when [K+] was raised in the presence of choline chloride (50 microM), arguing that MEPC changes were not primarily due to a lower and less uniform vesicular filling. Channel kinetics were not altered by high [K+]o, since the time constant of decay of miniature end-plate currents (TMEPC-s) did not change. Acetylcholine clearance from the synaptic cleft, however, appeared to be faster in high [K+]o since with cholinesterase blocked throughout, TMEPC-s were shortened. The changes of spontaneous quantal discharge induced by high [K+]o can be almost entirely explained by altered spatial distribution of vesicular release if, as recent reports suggest, at high [K+]o, exocytosis appears randomly not only at but also in between the active zones. However, relatively greater frequency of large MEPCs suggests that in high [K+]o some, and possibly all, quanta are filled above normal levels. High [Ca2+]o appears to counteract, although not always completely, all changes in spontaneous quantal secretion induced by high [K+]o. It is possible that high [Ca2+]o reverses the changes in the spatial distribution of vesicular release induced by high [K+]o. However, high [Ca2+]o also leads to other pre- and postsynaptic changes.
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PMID:Changes in miniature end-plate currents due to high potassium and calcium at the frog neuromuscular junction. 326 41

Spontaneous release of acetylcholine (ACh) from rat basal forebrain slices in the presence of cholinesterase inhibitor was directly determined using a specific radioimmunoassay for ACh. The release was calcium dependent. A consistent amount of ACh release was observed throughout the experiment. Atropine (10(-8) to 10(-5) M) and pirenzepine (10(-7) to 10(-5) M) enhanced spontaneous ACh release. These findings indicate the presence of an M1 muscarinic autoreceptor that modulates spontaneous release of ACh in the rat basal forebrain.
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PMID:Presynaptic M1 muscarinic receptor modulates spontaneous release of acetylcholine from rat basal forebrain slices. 334 Mar 27

In the lichen Parmelia caperata (L.) Ach. the distribution pattern of membrane-bound Ca2+ is investigated in the symbionts by chlorotetracycline (CTC)-induced fluorescence during the development of propagative structures, the soredia. The results demonstrate that Ca2+ accumulation in the alga and the fungus is associated with this morphogenetic process; particularly, polarized hyphal growth involves a tip-to-base Ca2+ gradient. CTC fluorescence distribution is coincident with that of cholinesterase (ChE) activity during morphogenesis of soredia. A comparison is suggested with 'embryonic ChE' of animal cells, where developmental events are regulated by a cholinergic mechanism that also modulates Ca2+ levels.
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PMID:Membrane-bound Ca2+ distribution visualized by chlorotetracycline fluorescence during morphogenesis of soredia in a lichen. 339

The effects of Y-8894 on experimental amnesia in rats induced by transient cerebral ischemia (600 sec) according to the method of Pulsinelli and Brierley were studied using the one trial passive avoidance response and the pole climbing discrete avoidance response. All drugs were administered to the rats immediately after recirculation. The following results were obtained: 1) In the one trial passive avoidance response test, Y-8894 (2.5, 5 and 10 mg/kg, i.p.) improved significantly the decreased latency induced by the ischemia, and it was most effective at 5 mg/kg. Calcium-hopantenate (100, 250 and 500 mg/kg, i.p.) and dihydroergotoxine (5 and 10 mg/kg, i.p.) tended to increase the latency. On the other hand, physostigmine (0.025, 0.05 and 0.1 mg/kg, i.p.), a cholinesterase inhibitor, increased the latency significantly, and it was most effective at 0.05 mg/kg. 2) The pole climbing discrete avoidance response was significantly decreased by the ischemia compared with the sham operated group, and Y-8894 (5 mg/kg, i.p.) tended to improve this decreased avoidance response. 3) Y-8894 (5 mg/kg, i.p.) facilitated recovery from the changes in glycolytic metabolism, and inhibited the accumulation of choline due to the dysfunction of the neuronal membranes induced by the ischemia. These results show that Y-8894 has beneficial effects on experimental amnesia induced by transient cerebral ischemia.
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PMID:[Pharmacological studies on Y-8894. (VII). Effects on transient cerebral ischemia-induced amnesia in rats]. 344 14

The aim of the study is to follow up the changes in auditory and vestibular systems, common interactions between the sensory systems and the changes in some biochemical indices after vestibular loading in drivers. Several groups of drivers of heavy freight trucks were studied, aged from 25-60 and a length of service from 5 to 30 years, according to a standard programme for otoneurological examination and application of modern otoneurological methods. The biochemical investigations were performed to 32 healthy and 19 sick drivers with vestibular disorders, prior to and post vestibular provocation. The following biochemical indices were studied: serotonin, histamine, cholinesterase activity, glucose, GOT, GPT, alkaline phosphatase, calcium, potassium, sodium, chlorides, inorganic phosphorus. The biochemical changes, associated with vestibular loading of organism were established not to be strongly manifested and coming out of the frames of the normal values, nevertheless, they are significant for a given subject and should not be neglected. The data are of importance in the vocational selection of driver-applicants, prophylaxis and treatment of those working under stress situations and extreme impacts.
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PMID:[Otoneurological and biochemical research on the drivers of motor vehicles]. 349 83

The active zone is a unique presynaptic membrane specialization that is believed to be the site of neurotransmitter release. To examine directly the relationship between active zone ultrastructure and synaptic efficacy, frog neuromuscular junctions were studied with a new technique combining electrophysiology, light microscopy, and freeze-fracture of identified single muscle fibers. This technique allows correlations to be made between quantal content (measured in low Ca2+ and high Mg2+ Ringer solution), endplate size, and active zone structure at the same neuromuscular junctions. By measuring physiological and morphological variables at the same junctions, the validity of structure-function correlations is significantly improved. Synaptic quantal content in 91 physiologically identified muscle fibers varied considerably and was only poorly correlated with endplate size, as shown in previous studies. To measure the total length of endplate branches, either a modified cholinesterase stain or rhodamine-labeled peanut agglutinin stain was used. When the same identified muscle fibers were freeze-fractured, active zones were exposed in 17 junctions. In a replica that contained a large part of one nerve terminal, there was no detectable gradient in active zone structure along the length of 3 different nerve terminal branches identifiable with both light and electron microscopy. The results from these 17 identified junctions indicate that quantal content per unit terminal length is positively correlated with the amount of active zone per unit terminal length. The estimated total active zone length and total number of active zone particles per junction are also positively correlated with the quantal content in these identified junctions. This study suggests that active zone size and spacing are better indicators of transmitter release than is endplate size and that the active zone may play an important role in regulating synaptic efficacy at the neuromuscular junction.
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PMID:Correlations between active zone ultrastructure and synaptic function studied with freeze-fracture of physiologically identified neuromuscular junctions. 350 Feb 82

The effect of diisopropyl fluorophosphate (DFP), a potent cholinesterase (ChE) inhibitor, on loading quin 2 acetoxymethyl ester (quin 2/AM) and fura 2/AM into smooth muscle cells isolated from guinea pig taenia coli was investigated spectrofluorometrically. The presence of DFP during the loading permitted the incorporation of quin 2 into the cells, so that it became possible to measure intracellular Ca2+ concentrations using the ester of this dye. Also, DFP significantly enhanced the incorporation of fura 2 into the cells. These results indicate that loading of quin 2/AM and fura 2/AM into the smooth muscle cells may depend on the suppression of ChE or various serine protease activities outside cells.
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PMID:Effect of DFP on loading of fura 2/AM and quin 2/AM into single smooth muscle cells prepared from guinea pig taenia coli. 360 23


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