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Effects of urapidil on 5-hydroxytryptamine induced platelet aggregation and on 14C-5-hydroxytryptamine uptake in
Abstract:
Urapidil inhibits the 5HT induced human platelet aggregation and the 5HT uptake by platelets in vitro and ex vivo. The aggregation was inhibited with a KI-value of 8.8 microM and the 5HT uptake in a noncompetitive way with KI1 = 15.3 microM and K12 = 10.6 microM. In vivo, the 5HT induced platelet aggregation was increased 4 h after oral administration of 60 mg urapidil. Subsequently, the aggregation decreased and reached a minimum at various times in the different volunteers. Eight h after oral administration of 60 mg urapidil, the 5HT uptake velocity was reduced approximately 40%.