Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
4
|
| pubmed:dateCreated |
1986-5-30
|
| pubmed:abstractText |
[3H]NECA (1-(6-amino-9H-purin-9-yl)-1-deoxy-N-ethyl-beta-D-ribofuronamide) is known to bind to both the A1 and A2 subtypes of adenosine receptor in rat striatal membranes. In order to study the putative A2 component of [3H]NECA binding, we examined several compounds for the ability to selectively eliminate the A1 component of binding; N6-cyclopentyladenosine was found to give the most satisfactory results. Binding of [3H]NECA in the presence of 50 nM N6-cyclopentyladenosine was characterized. The rank order of potency for inhibition of [3H]NECA binding was NECA much greater than 2-chloroadenosine greater than N6-[(R)-1-methyl-2-phenyl-ethyl]adenosine (R-PIA) greater than N6-cyclohexyladenosine greater than S-PIA, indicating that binding was to an A2 adenosine receptor. When affinities of compounds in [3H]NECA binding to A2 receptors were compared to their affinities in [3H]N6-cyclohexyladenosine binding to A1 receptors, N6-cyclopentyladenosine was the most A1-sensitive agonist (A1 Ki, 0.59 nM; A2 Ki, 460 nM; Ki ratio, 780), whereas the selective coronary vasodilator 2-(phenylamino)adenosine was the most A2-selective agonist (A1, 560 nM; A2, 120 nM; ratio, 0.21). The antagonist 8-cyclopentyltheophylline had considerable A1 selectivity (A1, 11 nM; A2, 1400 nM; ratio, 130), whereas alloxazine had slight A2 selectivity (A1, 5200 nM; A2, 2700; ratio, 0.52). [3H]NECA binding to A2 receptors was highest in striatum but was detectable at much lower levels in each of seven other brain areas. The regional distribution of [3H]NECA binding and the affinities of adenosine agonists and antagonists for inhibition of binding indicate that the site labeled by [3H]NECA belongs to the high affinity, or A2a, subclass of A2 receptor.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-Chloroadenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Deaminase,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine-5'-(N-ethylcarboxamide),
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Ethylmaleimide,
http://linkedlifedata.com/resource/pubmed/chemical/N(6)-cyclohexyladenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylisopropyladenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Purinergic
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Apr
|
| pubmed:issn |
0026-895X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
29
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
331-46
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:3010074-2-Chloroadenosine,
pubmed-meshheading:3010074-Adenosine,
pubmed-meshheading:3010074-Adenosine Deaminase,
pubmed-meshheading:3010074-Adenosine-5'-(N-ethylcarboxamide),
pubmed-meshheading:3010074-Animals,
pubmed-meshheading:3010074-Corpus Striatum,
pubmed-meshheading:3010074-Cyclic AMP,
pubmed-meshheading:3010074-Ethylmaleimide,
pubmed-meshheading:3010074-Female,
pubmed-meshheading:3010074-Fibroblasts,
pubmed-meshheading:3010074-Humans,
pubmed-meshheading:3010074-Male,
pubmed-meshheading:3010074-Mathematics,
pubmed-meshheading:3010074-Phenylisopropyladenosine,
pubmed-meshheading:3010074-Rats,
pubmed-meshheading:3010074-Rats, Inbred Strains,
pubmed-meshheading:3010074-Receptors, Cell Surface,
pubmed-meshheading:3010074-Receptors, Purinergic,
pubmed-meshheading:3010074-Structure-Activity Relationship,
pubmed-meshheading:3010074-Tissue Distribution
|
| pubmed:year |
1986
|
| pubmed:articleTitle |
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
|
| pubmed:publicationType |
Journal Article
|