AustralieFrV1, Istex, Corpus, bibRecord, 001F68

Actions of thienyl analogs of baclofen in the guinea-pig isolated ileum

Identifieur interne : 001F68 ( Istex/Corpus ); précédent : 001F67; suivant : 001F69

Actions of thienyl analogs of baclofen in the guinea-pig isolated ileum

Auteurs : Jennifer Ong ; David I. B. Kerr ; Pascal Berthelot ; Claude Vaccher ; Nathalie Flouquet ; Michel Debaert

Source :

European Journal of Pharmacology [ 0014-2999 ] ; 1992.

RBID : ISTEX:A69CFD2618ED656CD762FB3C23E6B2B7E4BF0D14

English descriptors

KwdEn :
- Adelaide, Agonist, Analog, Baclofen, Berthelot, Bowery, Cholinergic, Cholinergic twitch contractions, Debaert, Ecs0, Ecs0 value, Gaba, Ileal, Ileal preparations, Ileum, Krebs solution, Naloxone, Prager, Receptor, Receptor agonists, Receptor sites, Substituent, Theophylline, Thienyl, Thienyl analogs.
Teeft :
- Adelaide, Agonist, Analog, Baclofen, Berthelot, Bowery, Cholinergic, Cholinergic twitch contractions, Debaert, Ecs0, Ecs0 value, Gaba, Ileal, Ileal preparations, Ileum, Krebs solution, Naloxone, Prager, Receptor, Receptor agonists, Receptor sites, Substituent, Theophylline, Thienyl, Thienyl analogs.

Abstract

Abstract: In guinea-pig isolated ileal preparations, the 5-methylthien-2-yl (5d), 5-bromothien-2-yl (5f) and 5-chlorothien-2-yl (5h) analogs of baclofen depressed twitch responses to field stimulation in a dose-dependent manner. These actions were reversibly and competitively antagonised by 2-hydroxysaclofen but not by naloxone, phentolamine, propranolol or theophylline. The relative potencies (EC50 values) were baclofen (10 μM) > 5h (40 μM) > 5d (80 μM) > 5f (120 μM). These analogs represent a novel class of specific GABAB receptor agonists which, like baclofen, should readily enter the brain.

Url:

https://api.istex.fr/document/A69CFD2618ED656CD762FB3C23E6B2B7E4BF0D14/fulltext/pdf

DOI: 10.1016/0014-2999(92)90189-B

Links to Exploration step

ISTEX:A69CFD2618ED656CD762FB3C23E6B2B7E4BF0D14

Le document en format XML

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<head><ce:dochead><ce:textfn>Short communication</ce:textfn>
</ce:dochead>
<ce:title>Actions of thienyl analogs of baclofen in the guinea-pig isolated ileum</ce:title>
<ce:author-group><ce:author><ce:given-name>Jennifer</ce:given-name>
<ce:surname>Ong</ce:surname>
<ce:cross-ref refid="AFF1"><ce:sup>1</ce:sup>
</ce:cross-ref>
<ce:cross-ref refid="COR1"><ce:sup>∗</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:author><ce:given-name>David I.B.</ce:given-name>
<ce:surname>Kerr</ce:surname>
<ce:cross-ref refid="AFF1"><ce:sup>1</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:author><ce:given-name>Pascal</ce:given-name>
<ce:surname>Berthelot</ce:surname>
<ce:cross-ref refid="AFF2"><ce:sup>a</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:author><ce:given-name>Claude</ce:given-name>
<ce:surname>Vaccher</ce:surname>
<ce:cross-ref refid="AFF2"><ce:sup>a</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:author><ce:given-name>Nathalie</ce:given-name>
<ce:surname>Flouquet</ce:surname>
<ce:cross-ref refid="AFF2"><ce:sup>a</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:author><ce:given-name>Michel</ce:given-name>
<ce:surname>Debaert</ce:surname>
<ce:cross-ref refid="AFF2"><ce:sup>a</ce:sup>
</ce:cross-ref>
</ce:author>
<ce:affiliation id="AFF1"><ce:label>1</ce:label>
<ce:textfn>Department of Anaesthesia and Intensive Care, University of Adelaide, Adelaide, South Australia 5000, Australia</ce:textfn>
</ce:affiliation>
<ce:affiliation id="AFF2"><ce:label>a</ce:label>
<ce:textfn>Laboratoire de Pharmacie Chimique, Faculté de Pharmacie, Université de Lille, Lille, France</ce:textfn>
</ce:affiliation>
<ce:correspondence id="COR1"><ce:label>∗</ce:label>
<ce:text>Correspondence to: J. Ong, Department of Anaesthesia and Intensive Care, University of Adelaide, Adelaide, South Australia 5000, Australia. Tel. 61.8.228 5163, fax 61.8 232 3283.</ce:text>
</ce:correspondence>
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<ce:date-received day="24" month="2" year="1992"></ce:date-received>
<ce:date-revised day="6" month="5" year="1992"></ce:date-revised>
<ce:date-accepted day="26" month="5" year="1992"></ce:date-accepted>
<ce:abstract><ce:section-title>Abstract</ce:section-title>
<ce:abstract-sec><ce:simple-para>In guinea-pig isolated ileal preparations, the 5-methylthien-2-yl (5d), 5-bromothien-2-yl (5f) and 5-chlorothien-2-yl (5h) analogs of baclofen depressed twitch responses to field stimulation in a dose-dependent manner. These actions were reversibly and competitively antagonised by 2-hydroxysaclofen but not by naloxone, phentolamine, propranolol or theophylline. The relative potencies (EC<ce:inf>50</ce:inf>
 values) were baclofen (10 μM) > 5h (40 μM) > 5d (80 μM) > 5f (120 μM). These analogs represent a novel class of specific GABA<ce:inf>B</ce:inf>
 receptor agonists which, like baclofen, should readily enter the brain.</ce:simple-para>
</ce:abstract-sec>
</ce:abstract>
<ce:keywords><ce:section-title>Keywords</ce:section-title>
<ce:keyword><ce:text>Baclofen</ce:text>
</ce:keyword>
<ce:keyword><ce:text>GABA<ce:inf>B</ce:inf>
 receptor agonists</ce:text>
</ce:keyword>
<ce:keyword><ce:text>Thienyl baclofen analogs</ce:text>
</ce:keyword>
<ce:keyword><ce:text>2-Hydroxysaclofen</ce:text>
</ce:keyword>
<ce:keyword><ce:text>Ileum (guinea-pig, isolated)</ce:text>
</ce:keyword>
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<name type="personal"><namePart type="given">Jennifer</namePart>
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<affiliation>Department of Anaesthesia and Intensive Care, University of Adelaide, Adelaide, South Australia 5000, Australia</affiliation>
<affiliation>Correspondence to: J. Ong, Department of Anaesthesia and Intensive Care, University of Adelaide, Adelaide, South Australia 5000, Australia. Tel. 61.8.228 5163, fax 61.8 232 3283.</affiliation>
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<name type="personal"><namePart type="given">David I.B.</namePart>
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<name type="personal"><namePart type="given">Pascal</namePart>
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<name type="personal"><namePart type="given">Claude</namePart>
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<name type="personal"><namePart type="given">Nathalie</namePart>
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<name type="personal"><namePart type="given">Michel</namePart>
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<abstract lang="en">Abstract: In guinea-pig isolated ileal preparations, the 5-methylthien-2-yl (5d), 5-bromothien-2-yl (5f) and 5-chlorothien-2-yl (5h) analogs of baclofen depressed twitch responses to field stimulation in a dose-dependent manner. These actions were reversibly and competitively antagonised by 2-hydroxysaclofen but not by naloxone, phentolamine, propranolol or theophylline. The relative potencies (EC50 values) were baclofen (10 μM) > 5h (40 μM) > 5d (80 μM) > 5f (120 μM). These analogs represent a novel class of specific GABAB receptor agonists which, like baclofen, should readily enter the brain.</abstract>
<note type="content">Section title: Short communication</note>
<subject><genre>Keywords</genre>
<topic>Baclofen</topic>
<topic>GABAB receptor agonists</topic>
<topic>Thienyl baclofen analogs</topic>
<topic>2-Hydroxysaclofen</topic>
<topic>Ileum (guinea-pig, isolated)</topic>
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<dateIssued encoding="w3cdtf">19920806</dateIssued>
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<identifier type="ISSN">0014-2999</identifier>
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<caption>vol.</caption>
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<detail type="issue"><number>2–3</number>
<caption>no.</caption>
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Actions of thienyl analogs of baclofen in the guinea-pig isolated ileum

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