Abstract
Newly synthesized mono-, di-, and triphosphate of 2-alkynyl adenosines showed very different behavior in human platelet P2Y receptor models, according to the different alkynyl chains. In fact, 2-hexynyladenosine di- (5) and triphosphate (7) induced platelet shape change and aggregation and inhibited PGE(1)-induced increase in platelet cyclic AMP. On the contrary, the corresponding 2-phenylethynyladenosine di- (6) and triphosphate (8) did not induce platelet shape change or aggregation, but inhibited platelet aggregation induced by ADP.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine / analogs & derivatives*
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Adenosine / chemical synthesis*
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Adenosine / chemistry
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Adenosine / pharmacology
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Alkynes / chemical synthesis*
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Alkynes / chemistry
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Alkynes / pharmacology
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Blood Platelets / cytology
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Blood Platelets / drug effects*
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Blood Platelets / physiology
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Cell Shape / drug effects
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Cyclic AMP / antagonists & inhibitors
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Cyclic AMP / biosynthesis
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Humans
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In Vitro Techniques
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Membrane Proteins / agonists
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Membrane Proteins / drug effects*
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Membrane Proteins / physiology
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Organophosphates / chemical synthesis*
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Organophosphates / chemistry
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Organophosphates / pharmacology
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / chemical synthesis*
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / pharmacology
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Purinergic P2 Receptor Agonists
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2 / drug effects*
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Receptors, Purinergic P2 / physiology
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Receptors, Purinergic P2Y1
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Receptors, Purinergic P2Y12
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Structure-Activity Relationship
Substances
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Alkynes
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Membrane Proteins
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Organophosphates
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P2RY1 protein, human
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P2RY12 protein, human
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Platelet Aggregation Inhibitors
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Purinergic P2 Receptor Agonists
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2
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Receptors, Purinergic P2Y1
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Receptors, Purinergic P2Y12
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2-hexynyladenosine
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Cyclic AMP
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Adenosine