Linked Life Data

2795461

Source:http://linkedlifedata.com/resource/pubmed/id/2795461

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1989-11-7
pubmed:abstractText
A series of adenosine A2 receptor agonists were examined for their ability to activate adenosine A2 receptors and inhibit nucleoside transport. A2 receptor activation was measured by the ability of these adenosine agonists to relax porcine coronary smooth muscle, where the compounds varied in their EC50 values from 4.5 nM (CGS 21680A (2-[p-(2-carboxyethyl) phenylethylamino]-5'-N-ethylcarboxamidoadenosine)] to 3.6 microM (CGS 23321 [2 alpha,3 alpha-dihydroxy-1 beta-hydroxymethyl-4 beta-(2-phenylamino-9- adenyl)-cyclopentane]). Nucleoside transport was measured as the nitrobenzylthioinosine-sensitive cellular accumulation of [3H]uridine into guinea pig erythrocytes at 22 degrees C. The initial velocity of transport was dependent on substrate concentration and a substrate-velocity curve yielded a Km of 78 +/- 16 microM and a Vmax of 0.31 +/- 0.049 mmol/l of cell water per hr (mean +/- S.D., n = 4). Dipyridamole, a known potent inhibitor of nucleoside transport, blocked cellular [3H]uridine accumulation with an EC50 of 29.4 nM. Whereas a number of the adenosine agonists tested showed little or no inhibition of nucleoside transport, CV 1808 (2-phenylaminoadenosine) inhibited transport with an EC50 of 140 nM. In addition, two carbocyclic derivatives of CV 1808, CGS 23321 and CGS 23302 [(-)2S,3R-dihydroxy-4R-hydroxymethyl-1R-[2-(p-ethoxycarbonyl)- phenylamino-9-adenyl]-cyclopentane) inhibited nucleoside transport with respective EC50 values of 366 and 168 nM. The data suggest that these compounds have a different structure-activity relationship for adenosine A2 receptors and for the site mediating nucleoside transport inhibition.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
251
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
279-87
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Effects of adenosine A2 receptor agonists on nucleoside transport.
pubmed:affiliation
Research Department, Ciba-Geigy Corporation, Summit, New Jersey 07901.
pubmed:publicationType
Journal Article, In Vitro