2-(6-carboxyhexyl)cyclopentanone hexylhydrazone: a potent inhibitor of the blood platelet cyclo-oxygenase

G C Le BretonD L Venton


Previous studies have demonstrated that 13-azaprostanoic acid (13-APA) is a potent and specific antagonist of thromboxane A2/prostaglandin H2 (TXA2/PGH2) at the platelet receptor level. In the present study we evaluated the effects of a new azaprostanoid , 2-(6- carboxyhexyl ) cyclopentanone hexylhydrazone (CPH), on human platelet function. This hydrazone was found to completely inhibit arachidonic acid (AA)-induced platelet aggregation at 1 microM CPH. On the other hand, CPH was not an effective inhibitor of PGH2-induced aggregation. Furthermore, 100 microM CPH was completely ineffective in blocking platelet aggregation stimulated by adenosine diphosphate (ADP) or the stable prostaglandin endoperoxide analog U46619 (which presumably acts at the TXA2/PGH2 receptor). Measurement of platelet thromboxane B2 (TXB2) production demonstrated tha the primary site-of-action of CPH is at the cyclo-oxygenase level. Thus, CP inhibited TXB2 formation from AA in a dose-dependent manner (0.1 microM-100 microM CPH)2. In contrast, CPH blocked TXB2 production from PGH2 only at the highest CPH concentration tested, i.e., 100 microM. These results indicate that relative to 13-APA, addition of a second nitrogen at C14 and a double bond between the ...Continue Reading


Jul 1, 1979·Journal of Medicinal Chemistry·D L VentonG C Le Breton
Apr 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·P NeedlemanM Minkes
Aug 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·G C Le BretonP V Halushka
Sep 1, 1977·Analytical Biochemistry·F A FitzpatrickF F Sun
Jun 23, 1971·Nature: New Biology·J B Smith, A L Willis

Related Concepts

2-(6-carboxyhexyl)cyclopentanone hexylhydrazone
Eicosatetraenoic Acids
Blood Platelets
Dose-Response Relationship, Drug
Saturated Fat
Platelet Aggregation
Prostaglandin Endoperoxides, Synthetic
Prostaglandins H
Prostanoic Acids
Thromboxane B2

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