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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
7
|
| pubmed:dateCreated |
1998-2-5
|
| pubmed:abstractText |
1. In the present study, we investigated the ability of a recently introduced non-xanthine A2A receptor antagonist, ZM241385 (4-(2-[7-amino-2-(2-furyl[1,2,4]-triazolo[2,3-a[1,3,5]triazin-5-yl -aminoethyl)phenol) to displace binding of the prototypical A2A adenosine receptor agonist [3H]CGS21680 (2-[4-(2-p-carboxyethyl)phenylamino]-5'-N-ethylcarboxamidoadenosine) and to modify the facilitatory responses caused by the A2A selective agonists, CGS21680 and HENECA (2-hexynl-5'-N-ethylcarboxamidoadenosine) in rat hippocampal preparations. 2. ZM241385 was nearly equipotent to displace [3H]CGS21680 (30 nM) binding to hippocampal (Ki of 0.52 nM) and to striatal membranes (Ki of 0.35 nM), whereas HENECA was a more potent displacer of [3H]CGS21680 binding to striatal (Ki of 4.5 nM) than to hippocampal membranes (Ki of 19 nM). 3. HENECA (3-30 nM) was equipotent with CGS21680 to facilitate veratridine-evoked [3H]acetylcholine release from superfused hippocampal synaptosomes and ZM241385 (20 nM) inhibited the facilitatory effects of both HENECA (30 nM) and CGS21680 (30 nM); this antagonism was mimicked by CSC (250 nM). 4. In contrast, CGS21680 (10-30 nM) was more potent than HENECA (10-30 nM) to facilitate synaptic transmission in Schaffer fibres/CA1 pyramid synapses of hippocampal slices and the facilitatory effect of CGS21680 (10 nM) was blocked by ZM241385 (20 nM) whereas CSC (250 nM) caused a 40% attenuation of this CGS21680-induced facilitation. 5. These results indicate that ZM241385 is the first A2A antagonist with equal potency to displace [3H]CGS21680 binding to striatal and limbic regions, and with general efficiency to antagonize HENECA- or CGS21680-mediated facilitatory responses in the hippocampus.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-(4-(2-carboxyethyl)phenethylamino)...,
http://linkedlifedata.com/resource/pubmed/chemical/2-hexynyladenosine-5'-N-ethylcarboxa...,
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine-5'-(N-ethylcarboxamide),
http://linkedlifedata.com/resource/pubmed/chemical/Antihypertensive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Phenethylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Aggregation Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Purinergic P1 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Triazines,
http://linkedlifedata.com/resource/pubmed/chemical/Triazoles,
http://linkedlifedata.com/resource/pubmed/chemical/ZM 241385
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Dec
|
| pubmed:issn |
0007-1188
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
122
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1279-84
|
| pubmed:dateRevised |
2010-11-18
|
| pubmed:meshHeading |
pubmed-meshheading:9421273-Acetylcholine,
pubmed-meshheading:9421273-Adenosine,
pubmed-meshheading:9421273-Adenosine-5'-(N-ethylcarboxamide),
pubmed-meshheading:9421273-Animals,
pubmed-meshheading:9421273-Antihypertensive Agents,
pubmed-meshheading:9421273-Binding Sites,
pubmed-meshheading:9421273-Hippocampus,
pubmed-meshheading:9421273-Ligands,
pubmed-meshheading:9421273-Membranes,
pubmed-meshheading:9421273-Phenethylamines,
pubmed-meshheading:9421273-Platelet Aggregation Inhibitors,
pubmed-meshheading:9421273-Purinergic P1 Receptor Agonists,
pubmed-meshheading:9421273-Rats,
pubmed-meshheading:9421273-Synaptic Transmission,
pubmed-meshheading:9421273-Synaptosomes,
pubmed-meshheading:9421273-Triazines,
pubmed-meshheading:9421273-Triazoles,
pubmed-meshheading:9421273-Visual Cortex
|
| pubmed:year |
1997
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| pubmed:articleTitle |
ZM241385 is an antagonist of the facilitatory responses produced by the A2A adenosine receptor agonists CGS21680 and HENECA in the rat hippocampus.
|
| pubmed:affiliation |
Department of Chemistry & Biochemistry, Faculty of Sciences, University of Lisbon, Campo Grande, Portugal.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|