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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
1995-3-3
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pubmed:abstractText |
Release-regulating gamma-aminobutyric acidB (GABAB) autoreceptors were studied in synaptosomes from fresh specimens of human cerebral cortex. The K+ (12 mM)-evoked overflow of [3H]GABA was inhibited by the GABAB receptor agonists (-)-baclofen (EC50 = 1.48 microM) and 3-aminopropylphosphinic acid (3-APPA; EC50 = 0.034 microM). The effect of 10 microM (-)-baclofen was differentially reduced by the three GABAB receptor antagonists CGP 52432 ([3-[[(3,4-dichlorophenyl)methyl)amino]propyl]-(diethoxymethyl)- phosphinic acid), phaclofen and CGP 35348 (3-aminopropyl-(diethoxymethyl)- phosphinic acid). CGP 52432 was by far the most potent antagonist (IC50 = 0.09 microM). Phaclofen was about 700-fold less potent than CGP 52432 (IC50 = 70.0 microM) while CGP 35348 was ineffective up to 100 microM. The present results suggest that human and rat GABAB neocortical autoreceptors have similar pharmacological characteristics.
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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/3-aminopropylphosphinic acid,
http://linkedlifedata.com/resource/pubmed/chemical/Baclofen,
http://linkedlifedata.com/resource/pubmed/chemical/Benzylamines,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 35348,
http://linkedlifedata.com/resource/pubmed/chemical/CGP 52432,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/GABA-A Receptor 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/Organophosphorus Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphinic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-B,
http://linkedlifedata.com/resource/pubmed/chemical/phaclofen
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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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 |
3
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pubmed:volume |
263
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
311-4
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:7843269-Adolescent,
pubmed-meshheading:7843269-Adult,
pubmed-meshheading:7843269-Aged,
pubmed-meshheading:7843269-Animals,
pubmed-meshheading:7843269-Baclofen,
pubmed-meshheading:7843269-Benzylamines,
pubmed-meshheading:7843269-Binding, Competitive,
pubmed-meshheading:7843269-Brain Neoplasms,
pubmed-meshheading:7843269-Cerebral Cortex,
pubmed-meshheading:7843269-Female,
pubmed-meshheading:7843269-GABA Agonists,
pubmed-meshheading:7843269-GABA Antagonists,
pubmed-meshheading:7843269-GABA-A Receptor Antagonists,
pubmed-meshheading:7843269-GABA-B Receptor Agonists,
pubmed-meshheading:7843269-GABA-B Receptor Antagonists,
pubmed-meshheading:7843269-Humans,
pubmed-meshheading:7843269-Male,
pubmed-meshheading:7843269-Middle Aged,
pubmed-meshheading:7843269-Organophosphorus Compounds,
pubmed-meshheading:7843269-Phosphinic Acids,
pubmed-meshheading:7843269-Rats,
pubmed-meshheading:7843269-Receptors, GABA-B
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pubmed:year |
1994
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pubmed:articleTitle |
Characterization of the GABA autoreceptor in human neocortex as a pharmacological subtype of the GABAB receptor.
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pubmed:affiliation |
Institute of Pharmacology and Pharmacognosy, University of Genoa, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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