Antiplatelet properties of AD 6 (8-monochloro-3-β-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin) have been studied in vitro and in vivo. The drug showed a marked inhibitory effect on platelet aggregation, β-thromboglobulin (βTG) release and thromboxane B2 (TxB2) production in vitro. However, such effects were seen only in the presence of high concentrations of the drug (10-3 and 10-4 mol/l) and completely disappeared at lower concentrations. No effect was seen in vivo following oral administration of 300 mg of the drug in a small group of volunteers. It can be concluded that in vitro properties of the drug cannot be surmised without due caution to indicate its potential clinical use.
Lack of antiplatelet activity of the new coumarin derivative 8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin under in vivo conditions in man.
FABRIS, FABRIZIO;
1986
Abstract
Antiplatelet properties of AD 6 (8-monochloro-3-β-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin) have been studied in vitro and in vivo. The drug showed a marked inhibitory effect on platelet aggregation, β-thromboglobulin (βTG) release and thromboxane B2 (TxB2) production in vitro. However, such effects were seen only in the presence of high concentrations of the drug (10-3 and 10-4 mol/l) and completely disappeared at lower concentrations. No effect was seen in vivo following oral administration of 300 mg of the drug in a small group of volunteers. It can be concluded that in vitro properties of the drug cannot be surmised without due caution to indicate its potential clinical use.
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