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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1996-10-24
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pubmed:abstractText |
In the guinea-pig isolated ileum, (RS)-(+/-)-baclofen induced a depression of cholinergic twitch contractions, reversibly and competitively antagonised by (S)-2-hydroxysaclofen (pA2 = 5.2 +/- 0.2), but not by (R)-2-hyroxysaclofen. The depression of excitatory field potentials by baclofen ( 5 mu M) in rat CA1 hippocampal slices was antagonised by (S)-2-hydroxysaclofen (100 mu m) (pA2 = 4.3), whilst in rat neocortex, (S)-2-hyroxysaclofen (50-500 mu M) antagonised the baclofen (10 mu M)-induced suppression of spontaneous discharges, the (R)-enantiomer being inactive. These results show that (S)-2-hydroxysaclofen is the active antagonist at central and peripheral GABAB receptors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
12
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pubmed:volume |
287
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
185-9
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:8749034-Animals,
pubmed-meshheading:8749034-Baclofen,
pubmed-meshheading:8749034-Dose-Response Relationship, Drug,
pubmed-meshheading:8749034-Guinea Pigs,
pubmed-meshheading:8749034-Hippocampus,
pubmed-meshheading:8749034-Ileum,
pubmed-meshheading:8749034-Male,
pubmed-meshheading:8749034-Membrane Potentials,
pubmed-meshheading:8749034-Muscle Contraction,
pubmed-meshheading:8749034-Rats,
pubmed-meshheading:8749034-Rats, Sprague-Dawley,
pubmed-meshheading:8749034-Receptors, GABA-B
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pubmed:year |
1995
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pubmed:articleTitle |
The (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations.
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pubmed:affiliation |
Department of Anaesthesia and Intensive Care, The University of Adelaide, Adelaide, South Australia 5005, Australia.
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pubmed:publicationType |
Journal Article
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