Studies on antiplatelet effect of OP-41483, a prostaglandin I2 analog, in experimental animals. 1. Effect on platelet function and thrombosis.

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概要

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• Anti platelet and antithrombotic effects of OP-41483, a PG1<SUB>21</SUB> analog, were studied in experimental animals, and the following results were obtained: 1) With 10 min-intravenous infusion to guinea pigs, OP-41483 inhibited platelet adhesiveness and platelet aggregation at 300-1000 ng/kg/min and 1000 ng/kg/ min, respectively. In these effects, OP-41483 was 1-3 times more potent than carbacyclin and 3 times less potent than PGI<SUB>2</SUB>. 2) With oral administration to guinea pigs, OP-41483 given as its α-cyclodextrin clathrate (OP-41483 α-CD) inhibited platelet adhesiveness at doses higher than 1.0 mg/kg (expressed in terms of OP-41483), whereas PGI<SUB>2</SUB> and carbacyclin did not at 10 mg/kg. OP-41483 α-CD also inhibited platelet aggregation after a single dose of 3 mg/kg and repeated doses of 3 mg/kg/day for 7 days. 3) In the electrically induced thrombosis model of guinea pig mesenteric artery, OP-41483 (300-1000 ng/kg/min, i.v.-infusion) and OP-41483 α-CD (1.0-3.0 mg/kg, p.o.) inhibited thrombus formation, but heparin (1.0-10 U, /kg/min, i.v.-infusion) did not. 4) In the rabbit extracorporeal circulation thrombosis model, OP-41483 (100 and 300 ng/kg/min, i.v.-infusion) inhibited thrombus formation in the extracorporeal shunt and prevented the decrease in platelet count, hematocrit and fibrinogen level in circulating blood. Heparin (1.0-3.0 U/kg/min, i.v.-infusion) also inhibited the thrombus formation and the decrease in fibrinogen level, but did not inhibit the decrease in hematocrit and platelet count.

• 公益社団法人 日本薬理学会の論文

著者

• Fujitani Buichi

  Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• WAKITANI Korekiyo

  Research Institute, Ono Pharmaceutical Co., Ltd.

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• Studies on antiplatelet effect of OP-41483, a prostaglandin I2 analog, in experimental animals. 1. Effect on platelet function and thrombosis.
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• Studies on antiplatelet effects of OP-41483, a prostaglandin l2 analog, in experimental animals II. Mechanism of its antiplatelet effect.

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