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Title: Effectiveness and tolerability of CV-3988, a selective PAF antagonist, after intravenous administration to man
Authors: Arnout, Jozef ×
Van Hecken, Anne
De Lepeleire, I
Miyamoto, Y
Holmes, I
De Schepper, Paul
Vermylen, Jozef #
Issue Date: Jul-1988
Series Title: British journal of clinical pharmacology vol:25 issue:4 pages:445-51
Abstract: 1. The efficacy and tolerability of CV-3988, a selective PAF antagonist with structural analogies with PAF, were studied after intravenous infusion in man. 2. The compound, in doses from 750 to 2,000 micrograms kg-1, significantly reduced platelet sensitivity for PAF. The threshold aggregating concentration (TAC) of PAF, expressed in % of the mean predosing value, increased in a dose dependent manner reaching 356 +/- 162% of the basal TAC at the end and 266 +/- 123% of the basal TAC 4 h after infusion of the highest dose. The TAC of PAF returned to the basal value within 24 h after the end of the infusion. 3. CV-3988 did not cause major side effects nor changes in blood pressure, pulse and respiratory rate. However, small but clinically insignificant changes in plasma haemoglobin and serum haptoglobin were seen at the end and 4 h after the end of the infusion, indicating a slight haemolysis. 4. Our results indicate that, when adequate infusion volumes and infusion rates are used, CV-3988 can safely be administered to man and should be useful in elucidating the role of PAF in disease.
ISSN: 0306-5251
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular and Vascular Biology
Faculty of Medicine - miscellaneous
Biomedical Sciences Group Management - miscellaneous
Clinical Pharmacology Centre (-)
× corresponding author
# (joint) last author

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