Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Xylocaine and its derivatives act specifically at the neuromuscular junction within the concentration range 0.05 to 2.0 mM. The charged form is the active form of the drugs. There is no correlation between "local anesthetic" activity and effect at the junction. Like d-tubocurarine, these drugs have little or no effect on quantum content, acetylcholinesterase activity, or the passive impedance of the muscle fiber. Yet they produce end plate potentials characterized by a brief, early component and a late, greatly prolonged component, as does procaine. Analysis of these changes in time course suggests that the drugs have little or no effect before receptors are activated by acetylcholine, but cause a decreased and often greatly prolonged response. Clear structure-activity relations indicate that the receptor to which the drugs bind to produce the prolonged response can be the receptor for acetylcholine. Comparison of the effects of the drugs on the end plate potential and on the response to iontophoretically applied acetylcholine also shows that the effects of Xylocaine depend on the time course of receptor activation and are quite different from the effects of d-tubocurarine.
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PMID:Alteration by xylocaine (lidocaine) and its derivatives of the time course of the end plate potential. 431 45

A single direct injection of a local anesthetic, 0.5% bupivacaine hydrochloride (BPVC) (Marcaine), into rat soleus and extensor digitorum longus (EDL) muscles produced massive fiber necrosis with extensive phagocytosis followed by rapid regeneration, predominantly in the soleus. Since the sarcoplasmic reticulum (SR) was functionally disturbed by BPVC administration as confirmed by an in vitro study, the sarcolemmal lysis seen in the early phase of degeneration was not assumed to simply result from direct damage to the plasma membrane caused by BPVC. The extracellular fluid containing a high concentration of calcium (Ca) ions then permeated into the sarcoplasm through the defective membrane resulting in hyper-contracted myofibrils. Selective damage to the Z-line, an early sign of muscle degeneration, was shown by electron microscopy and SDS gel electrophoresis (preferential loss of alpha-actinin). Administration of leupeptin, a thiol protease inhibitor, proved to be ineffective in inhibiting the necrotic process, because the BPVC induced muscle fiber breakdown was probably too acute and fulminant to demonstrate the inhibitory effect upon the degenerative process. Well preserved satellite cells, peripheral nerves, and acetylcholinesterase activity, and the absence of fibrous tissue proliferation in this system may be responsible for the extremely rapid regeneration with complete muscle fiber type differentiation. Since the sequence of fiber breakdown induced by BPVC administration was similar to that of progressive muscular dystrophy, this chemical will be one of the most useful tools for studying the pathophysiology of fiber necrosis and regeneration in diseased muscle.
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PMID:Pathophysiology of muscle fiber necrosis induced by bupivacaine hydrochloride (Marcaine). 661 29

To examine the morphological sequence of regenerating fibers after myonecrosis in dystrophic muscles, 0.5 ml of 0.5% bupivacaine hydrochloride (BPVC) (Marcaine) solution, a local anesthetic with a cytotoxic effect on the muscle fibers, was injected directly into the dystrophic (line 413) and nondystrophic (line 412) posterior latissimus dorsi (PLD) muscles of young and adult chickens. Although the dystrophic muscles after BPVC injection showed a rapid recovery with a similar tempo to that of nondystrophic ones, they showed different morphological behavior in the early phase of regeneration, including marked variability in the size of fibers and in the intracytoplasmic enzyme activities of nicotinamide adenine dinucleotide, reduced-tetrazolium reductase (NADH-TR), acetylcholinesterase (AChE), and nonspecific esterase (NSE).
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PMID:Regenerative capability of skeletal muscle in chicken muscular dystrophy. 673 79

Previous studies showed that anaesthesia with the barbiturate Thiopental induces an increase in membrane fluidity and a decrease in acetylcholinesterase activity in syncytiotrophoblast plasma membranes (SPM) obtained from placentas after Cesarean section. The aim of the present work was to compare the effect of a local anaesthetic (bupivacaine hydrochloride, trade name Marcaine) on SPM in vivo and to establish whether the anaesthetic is still present in the membrane after tissue preparation. The acetylcholinesterase activity was lower in Marcaine-anaesthetized SPM (27 +/- 3 against 39 +/- 6 in the control). The Marcaine action on the SPM can be ascribed to a competitive inhibition, similar to that reported for Thiopental. Fluorescence studies of the order parameter P showed it to be higher in SPM obtained from control (0.253 +/- 0.012) than in SPM obtained from Marcaine-exposed membranes (0.240 +/- 0.015). The local anaesthetic is still present in the SPM after their preparation (20.1 ng per mg membrane protein). It appears that the local anaesthetic exhibits an effect similar to that of the general anaesthetic, apparently due to binding to the membrane.
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PMID:Local anaesthetic effects on trophoblast membrane fluidity. 848 67