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Vol. 69, No. 1, 2003
Issue release date: September 2003
Section title: Original Paper
Pharmacology 2003;69:44–50
(DOI:10.1159/000071266)

Effects of Camonagrel, a Selective Inhibitor of Platelet Thromboxane Synthase, on the Platelet-Subendothelium Interaction

Villalobos M.A. · De La Cruz J.P. · Escalante R. · Arrebola M.M. · Guerrero A. · Sánchez de la Cuesta F.
Departments of aHuman Anatomy and bPharmacology and Therapeutics, University of Málaga, School of Medicine, Málaga, Spain

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 11/8/2002
Accepted: 3/11/2003
Published online: 8/6/2003

Number of Print Pages: 7
Number of Figures: 4
Number of Tables: 4

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA

Abstract

The aim of this study was to compare the effects of a new thromboxane synthase inhibitor, camonagrel, on platelet aggregation and platelet-subendothelium interaction under flow conditions, in comparison with a standard thromboxane synthase inhibitor (dazoxiben) and a cyclooxygenase inhibitor (acetylsalicylic acid). With respect to platelet aggregation in whole blood, the 50% inhibitory concentrations (IC50) of camonagrel were between 318 and 797 µmol/l after induction with collagen and adenosine 5′-diphosphate, respectively. For inhibition of thromboxane B2 synthesis, the IC50 values were 868 ± 68 µmol/l; prostaglandin E2 was inhibited only by acetylsalicylic acid (IC50 for camonagrel >2,000 µmol/l), and the leukocyte 6-keto-PGF level was increased by camonagrel. The greatest reduction in percentage subendothelial surface occupied by platelets (mainly in the thrombi) after blood perfusion was seen after incubation with camonagrel in the range of concentrations that inhibited collagen-induced platelet aggregation. In conclusion, camonagrel reduced platelet-subendothelium interaction under flow conditions, showing this effect in a range of concentrations lower than in inhibition of platelet aggregation.


  

Author Contacts

J.P. De La Cruz, MD
Department of Pharmacology and Therapeutics
University of Málaga School of Medicine, Campus de Teatinos s/n
E–2907 Málaga (Spain)
Tel. +34 952 132567, Fax +34 952 131568, E-Mail jpcruz@uma.es

  

Article Information

Received: November 8, 2002
Accepted after revision: March 3, 2003
Number of Print Pages : 7
Number of Figures : 4, Number of Tables : 4, Number of References : 26

  

Publication Details

Pharmacology (International Journal of Experimental and Clinical Pharmacology)
Founded 1959 as ‘Medicina Experimentalis’, continued 1965–1967 as ‘Medicina et Pharmacologia Experimentalis’; Founder: R. Domenjoz (1959–1977); Successors: B.B. Brodie (1968–1977); K. Lederis (1973–1985); K.-F. Sewing (1978–1998); E.S. Vesell (1970–2000)

Vol. 69, No. 1, Year 2003 (Cover Date: September 2003)

Journal Editor: J. Donnerer, Graz; M.L. Billingsley, Hershey, Pa.; T. Iijima, Akita
ISSN: 0031–7012 (print), 1423–0313 (Online)

For additional information: http://www.karger.com/pha


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 11/8/2002
Accepted: 3/11/2003
Published online: 8/6/2003

Number of Print Pages: 7
Number of Figures: 4
Number of Tables: 4

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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