New NO-donors with antithrombotic and vasodilating activities, VIII: Benzothiazole-2(3H)-nitrosimines.
Thirty title compounds were prepared and tested for their antiplatelet activity in the Born-test. Five nitrosimines inhibit the aggregation induced by collagen in concentrations below 10 mumol/L halfmaximally. Four compounds were investigated in an in vivo thrombosis model. An inhibition of thrombosis between 29 and 53% was observed in mesenteric arterioles of rats 2 h after p.o. administration (60 mg/kg). The effect in venoles was less pronounced (10-22%). For one compound these effects could still be demonstrated 4 h after oral application.
Rehse
K
K
Institut für Pharmazie, Freien Universität Berlin, Dahlem.
Ciborski
T
T
Lüdtke
E
E
D000818:Animals; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D009602:Nitrosamines / Q000138:chemical synthesis* / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D005343:Fibrinolytic Agents; D009602:Nitrosamines; D010975:Platelet Aggregation Inhibitors; D013844:Thiazoles; D014665:Vasodilator Agents