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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1999-6-3
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pubmed:abstractText |
In rat neocortical slices maintained in Mg2+-free Krebs medium, baclofen depressed the rate of spontaneous discharges in a concentration-dependent manner (EC50 = 4.5 microM). This depression was reversibly antagonised by 5-(S,R)-hydroxymethyl-5-methylmorpholinyl-2-(R,S)-acetic acid (Sch 54679) and 2-(R,S)-5-[spirocyclopentyl]-morpholinyl-acetic acid (Sch 51324) (respective pA2 values of 5.8+/-0.15 and 5.4+/-0.2). In electrically-stimulated slices preloaded with [3H]gamma-aminobutyric acid (GABA), Sch 54679 (EC50 = 3 microM) was 2.3 times more potent than Sch 51324 (EC50 = 7 microM) in increasing [3H]GABA release through antagonism of GABA(B) autoreceptors. These structurally novel analogues may be pharmacologically useful for elucidating GABA(B) receptor functions.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Baclofen,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA-B Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA-B Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Morpholines,
http://linkedlifedata.com/resource/pubmed/chemical/NNC 711,
http://linkedlifedata.com/resource/pubmed/chemical/Neurotransmitter Uptake Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Nipecotic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Oximes,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/gamma-Aminobutyric Acid
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0014-2999
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
12
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pubmed:volume |
369
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
33-7
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:10204678-Animals,
pubmed-meshheading:10204678-Baclofen,
pubmed-meshheading:10204678-Dose-Response Relationship, Drug,
pubmed-meshheading:10204678-Electric Stimulation,
pubmed-meshheading:10204678-Electrophysiology,
pubmed-meshheading:10204678-GABA Agonists,
pubmed-meshheading:10204678-GABA Antagonists,
pubmed-meshheading:10204678-GABA-B Receptor Agonists,
pubmed-meshheading:10204678-GABA-B Receptor Antagonists,
pubmed-meshheading:10204678-Male,
pubmed-meshheading:10204678-Morpholines,
pubmed-meshheading:10204678-Neocortex,
pubmed-meshheading:10204678-Neurotransmitter Uptake Inhibitors,
pubmed-meshheading:10204678-Nipecotic Acids,
pubmed-meshheading:10204678-Oximes,
pubmed-meshheading:10204678-Rats,
pubmed-meshheading:10204678-Rats, Sprague-Dawley,
pubmed-meshheading:10204678-Tritium,
pubmed-meshheading:10204678-gamma-Aminobutyric Acid
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pubmed:year |
1999
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pubmed:articleTitle |
Antagonism of GABA(B) receptors by morpholino-2-acetic acid derivatives Sch 54679 and Sch 51324 in rat brain.
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pubmed:affiliation |
Department of Anaesthesia and Intensive Care, The University of Adelaide, South Australia, Australia. jong@medicine.adelaide.edu.au
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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