Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1994-12-1
pubmed:abstractText
We have investigated both in vivo and ex vivo antiaggregatory activity of three adenosine receptor agonists in the anesthetized rabbit: the non-selective, 5'-N-ethyl-carboxamidoadenosine (NECA), the selective adenosine A1 receptor agonist, 2-chloro-N6-cyclopentyladenosine (CCPA) and the new selective A2 receptor agonist, 2-hexynyl-NECA. The drugs were administered by 30-min intravenous infusion at a dose reducing mean blood pressure by 40-50%. NECA and CCPA also markedly decreased heart rate. In ex vivo experiments, NECA (10 micrograms/kg) and 2-hexynyl-NECA (10 micrograms/kg) maximally inhibited adenosine 5'-diphosphate (ADP)-induced platelet aggregation at the end of drug infusion by 26.7 +/- 2.9% and 25.2 +/- 3.5%, respectively. In in vivo studies, the inhibition of platelet aggregation was evaluated using the technique based on selective accumulation of 111In-labeled platelets in pulmonary microcirculation upon challenge with ADP 100 micrograms/kg. NECA (10 micrograms/kg) and 2-hexynyl-NECA (10 micrograms/kg) decreased peak values for platelet accumulation by 35.3 +/- 6.9% and 52.5 +/- 5.9% and the area under curve values by 37.7 +/- 8.7% and 41.2 +/- 12.0%, respectively. In comparison, CCPA (100 micrograms/kg) did not affect platelet responses to ADP in either of the experimental models. Thus, the present study clearly demonstrates for the first time the in vivo antiplatelet activity of adenosine A2 receptor agonists, whereas the adenosine A1 receptor agonist was inactive, in consonance with the in vitro data.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
23
pubmed:volume
259
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
43-9
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit.
pubmed:affiliation
Research Laboratories, Schering-Plough S.p.A., Comazzo, Milan, Italy.
pubmed:publicationType
Journal Article