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)

Rats were intoxicated with two different S-aminoalkyl-phosphonothioate cholinesterase inhibitors, viz. I-1 (S-diethylaminoethyl-O-cyclohexyl-methyl-phosphonothioate), which has a mixed central/peripheral mode of action, and I-2, the methiodide derivative of I-1, which acts almost solely peripherally. It was found that atropine did not have any beneficial effect on lethality in the case of an I-2 intoxication but did so, although only slightly, in the case of I-1. Therefore, the effect of atropine against I-1 intoxications must be mediated through central mechanisms, the peripheral parasympatholytic effect being negligible in counteracting lethality. Furthermore atropine antagonized the convulsions caused by intoxication with I-1. The oxime used as a reactivator of inhibited acetylcholinesterase, HI-6, was more effective than atropine against either organophosphate. In the case of an I-2 intoxication HI-6 proved extremely active. It is, therefore, concluded that HI-6 acts mainly peripherally. It was also found that HI-6 has a slight anticonvulsive action. The combination of HI-6 and atropine had a large synergistic effect in the case of I-1, but in the case of I-2 hardly any synergism was observed. Obviously, the combination of the oxime and atropine is particularly effective when the toxicant has a mixed central/peripheral action. In such intoxications the acetylcholinesterase reactivation in the respiratory neuromuscular synapse by the oxime is supplemented by the central action of atropine, which improves respiratory control at the level of the central nervous system.
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PMID:The synergism of atropine and the cholinesterase reactivator HI-6 in counteracting lethality by organophosphate intoxication in the rat. 198 59

Near-real-ime assay is anassay method that the whole process from sampling until results could be obtained in approximately Iess than one hour. The ElIman assay for acetyl cholinesterase (AChE) has near real-time potential due to its simplicity and fast assay time. The commercial acetylcholinesterase from Electrophorus electricus is well known for its uses in insecticides detection. A lesser known fact is AChE is also sensitive to heavy metals. A near real-time inhibitive assay for heavy metals using AChE from this source showed promising results. Several heavy metals such as copper, silver and mercury could be etected with IC50 values of1.212, 0.1185 and 0.097 mg I-1, respectively. The Limits of Detection (LOD) for copper, silver and mercury were 0.01, 0.015 and 0.01 mg I-1, respectively. TheLimits of quantitation (LOQ) or copper, silver and mercury were 0.196, 0.112 and 0.025 mg I-1, respectively. The LOQvalues for copper, silver and mercury were well below the maximum permissible limit for these metal ions as outlined by Malaysian Department of Environment. A polluted location demonstrated near real-time applicability of the assay with variation oftemporal levels of heavy metals detected. The results show that AChE from Electrophorus electricus has the potential to be used as a near real-time biomonitoring tool for heavy
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PMID:Development of an inhibitive assay using commercial Electrophorus electricus acetylcholinesterase for heavy metal detection. 2455 14