[Inhibitory activity of bencyclan on platelet aggregation in vitro and in vivo (author's transl)].
N-[3-(Benzyl-cycloheptyloxy)-propyl]-N,N-dimethyl-amine (bencyclan-hydrogenfumarate, Fludilat¿) inhibits spontaneously enhanced aggregation in the tests which detect a spontaneous aggregating activity (PAT I--III) in 10(-5) molar concentration. Bencyclan also inhibits platelet adhesiveness and ADP or collagen induced platelet aggregation. 10(-5) M of bencyclan induced a slight swelling of platelets 5 times 10(-4) Mol inhibited the formation of tentacles completely and transformed the platelets into small spheres if investigated with interference-phase contrast microscopy. It is likely that the morphologic changes induced by bencyclan are responsible for the inhibitory effect on the different platelet function tests in vitro. In vivo oral application of 300-600 mg of bencyclan per day did not inhibit platelet aggregation. In patients with enhanced aggregating tendency i.v. injection of 200-400 mg bencyclan led to a short-time inhibition of platelet aggregation which usually did not last for more than 1 h. No binding of 14C-labelled bencyclan to platelets was found. In vitro and in vivo some 14C-labelled bencyclan was bound to albumins.
D000244:Adenosine Diphosphate; D000284:Administration, Oral; D000418:Albumins / Q000378:metabolism; D001537:Bencyclane / Q000378:metabolism / Q000494:pharmacology*; D001792:Blood Platelets / Q000378:metabolism; D003094:Collagen; D003508:Cycloheptanes / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007275:Injections, Intravenous; D008722:Methods; D010426:Pentosan Sulfuric Polyester; D010974:Platelet Aggregation / Q000187:drug effects*; D011485:Protein Binding; D013997:Time Factors
D000418:Albumins; D003508:Cycloheptanes; D010426:Pentosan Sulfuric Polyester; D000244:Adenosine Diphosphate; D001537:Bencyclane; D003094:Collagen
Thrombozytenaggregationshemmende Wirkung von Bencyclan in vitro und in vivo