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THE ANTICHOLINESTERASE ACTIVITY OF MEFLOQUINE

Identifieur interne : 000539 ( Istex/Corpus ); précédent : 000538; suivant : 000540

THE ANTICHOLINESTERASE ACTIVITY OF MEFLOQUINE

Auteurs : L. Y. Lim ; M. L. Go

Source :

RBID : ISTEX:90AF1A401D73691500AE4A31E30FC7AB4B5D1659

English descriptors

Abstract

1. The characteristics of the inhibition of electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BChE) by the antimalarial agents mefloquine, chloroquine, amodiaquine and amopyroquine were determined. 2. The antimalarials were found to be non‐competitive inhibitors of both AChE and BChE. In both enzyme systems, inhibitory potencies were in the order amodiaquine > amopyroquine > chloroquine > mefloquine. 3. The low inhibitory potency of mefloquine may account in part for the appearance of gastrointestinal and central nervous system disturbances only at high doses of the drug.

Url:
DOI: 10.1111/j.1440-1681.1985.tb00904.x

Links to Exploration step

ISTEX:90AF1A401D73691500AE4A31E30FC7AB4B5D1659

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<givenNames>L. Y.</givenNames>
<familyName>Lim</familyName>
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<personName>
<givenNames>M. L.</givenNames>
<familyName>Go</familyName>
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<unparsedAffiliation>Department of Pharmacy, National University of Singapore, Republic of Singapore</unparsedAffiliation>
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<keyword xml:id="k1">4‐aminoquinoline antimalarials</keyword>
<keyword xml:id="k2">cholinesterase inhibition</keyword>
<keyword xml:id="k3">mefloquine.</keyword>
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<abstract type="main" xml:lang="en">
<title type="main">SUMMARY</title>
<p>1. The characteristics of the inhibition of electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BChE) by the antimalarial agents mefloquine, chloroquine, amodiaquine and amopyroquine were determined.</p>
<p>2. The antimalarials were found to be non‐competitive inhibitors of both AChE and BChE. In both enzyme systems, inhibitory potencies were in the order amodiaquine > amopyroquine > chloroquine > mefloquine.</p>
<p>3. The low inhibitory potency of mefloquine may account in part for the appearance of gastrointestinal and central nervous system disturbances only at high doses of the drug.</p>
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<title>THE ANTICHOLINESTERASE ACTIVITY OF MEFLOQUINE</title>
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<title>THE ANTICHOLINESTERASE ACTIVITY OF MEFLOQUINE</title>
</titleInfo>
<name type="personal">
<namePart type="given">L. Y.</namePart>
<namePart type="family">Lim</namePart>
<affiliation>Department of Pharmacy, National University of Singapore, Republic of Singapore</affiliation>
<role>
<roleTerm type="text">author</roleTerm>
</role>
</name>
<name type="personal">
<namePart type="given">M. L.</namePart>
<namePart type="family">Go</namePart>
<affiliation>Department of Pharmacy, National University of Singapore, Republic of Singapore</affiliation>
<affiliation>Correspondence address: Correspondence: Dr M. L. Go, Department of Pharmacy, National University of Singapore, Lower Kent Ridge Road, Republic of Singapore (0511).</affiliation>
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<dateIssued encoding="w3cdtf">1985-10</dateIssued>
<edition>Received 18 January 1985; revision received 17 April 1985</edition>
<copyrightDate encoding="w3cdtf">1985</copyrightDate>
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<abstract lang="en">1. The characteristics of the inhibition of electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BChE) by the antimalarial agents mefloquine, chloroquine, amodiaquine and amopyroquine were determined. 2. The antimalarials were found to be non‐competitive inhibitors of both AChE and BChE. In both enzyme systems, inhibitory potencies were in the order amodiaquine > amopyroquine > chloroquine > mefloquine. 3. The low inhibitory potency of mefloquine may account in part for the appearance of gastrointestinal and central nervous system disturbances only at high doses of the drug.</abstract>
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<identifier type="eISSN">1440-1681</identifier>
<identifier type="DOI">10.1111/(ISSN)1440-1681</identifier>
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