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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1995-3-22
|
| pubmed:abstractText |
[3H]-2-Methylthio-ADP ([3H]-2-MeS-ADP), a stable analogue of ADP bound to one type of specific binding sites on rat platelets (KD = 0.77 +/- 0.07 nM, Bmax = 160 +/- 11 fmol/10(8) cells). 2-MeS-ADP and ADP antagonized [3H]-2-MeS-ADP binding, showing respective Ki values of 1.4 +/- 0.1 nM and 486 +/- 78 nM. Clopidogrel, a potent and specific inhibitor of ADP-induced platelet aggregation partially inhibited (approximately 70% inhibition) the binding of [3H]-2-MeS-ADP at the same time it abrogated 2-MeS-ADP- and ADP-induced adenylyl cyclase inhibition and aggregation. A population of clopidogrel-resistant [3H]-2-MeS-ADP binding sites was detected on platelets from treated animals. These receptor sites (KD = 0.9 +/- 0.2 nM, Bmax = 47 +/- 5 fmol/10(8) platelets) which showed high affinity for both ADP and 2-MeS-ADP (Ki values in the nanomolar range) might be involved in the ADP-induced shape change, a clopidogrel-resistant ADP-induced event. Using clopidogrel which acts via a direct and irreversible inhibition of ADP binding to its adenylyl cyclase-coupled receptor sites on platelets, we were able to discriminate between two types of ADP receptor sites. The former which was clopidogrel-sensitive represented about 70% of the total [3H]-2-MeS-ADP receptors and was responsible for ADP-induced platelet aggregation and adenylyl cyclase inhibition. The latter which was not affected by clopidogrel might be involved in ADP-induced shape-change.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Oct
|
| pubmed:issn |
0049-3848
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
15
|
| pubmed:volume |
76
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
157-69
|
| pubmed:dateRevised |
2003-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:7863466-Adenosine Diphosphate,
pubmed-meshheading:7863466-Adenylate Cyclase,
pubmed-meshheading:7863466-Animals,
pubmed-meshheading:7863466-Binding Sites,
pubmed-meshheading:7863466-Blood Platelets,
pubmed-meshheading:7863466-Female,
pubmed-meshheading:7863466-Platelet Aggregation,
pubmed-meshheading:7863466-Rats,
pubmed-meshheading:7863466-Rats, Sprague-Dawley,
pubmed-meshheading:7863466-Signal Transduction,
pubmed-meshheading:7863466-Ticlopidine
|
| pubmed:year |
1994
|
| pubmed:articleTitle |
Evidence for the existence of two different ADP-binding sites on rat platelets.
|
| pubmed:affiliation |
Sanofi Recherche, Hemobiology Research Department, Toulouse, France.
|
| pubmed:publicationType |
Journal Article
|