Z-335, a new thromboxane A(2) receptor antagonist, prevents arterial thrombosis induced by ferric chloride in rats

Eur J Pharmacol. 2000 Aug 11;401(3):413-8. doi: 10.1016/s0014-2999(00)00434-9.

Abstract

We examined the antithrombotic effect of Z-335 ((+/-)-sodium [2-(4-chlorophenylsulfonylaminomethyl)indan-5-yl]acetate monohydrate), an orally active thromboxane A(2) receptor (TP-receptor) antagonist that ameliorates experimental gangrene, using a rat arterial thrombosis model. The thrombi were induced by topical application of 50% ferric chloride solution to the rats abdominal artery. Z-335 (0.3-3 mg/kg, p.o.) inhibited thrombus formation in a dose-dependent manner. The antithrombotic effect of Z-335 (1 and 3 mg/kg, p.o.) was almost equivalent with that of cilostazol (100 mg/kg, p.o.), a selective phosphodiesterase type III inhibitor. The effect of Z-335 (3 mg/kg, p.o.), but not cilostazol, persisted for 16 h. Z-335, but not cilostazol, inhibited platelet aggregation induced by U-46619 (a TP-receptor agonist, 9, 11-dideoxy-9alpha,11alpha-methanoepoxy prostaglandin F(2alpha)) for 16 h in rat whole blood. Histopathological examination also revealed that Z-335 prevented ferric chloride-induced thrombus formation. These results suggest that Z-335 may prevent ferric chloride-induced arterial thrombosis through its antiplatelet action by blocking TP-receptor activation.

MeSH terms

  • Administration, Oral
  • Animals
  • Aorta, Abdominal / drug effects
  • Aorta, Abdominal / pathology
  • Chlorides
  • Cilostazol
  • Dose-Response Relationship, Drug
  • Ferric Compounds / adverse effects*
  • Fibrinolytic Agents / pharmacology*
  • Indans / pharmacology*
  • Male
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Thromboxane / antagonists & inhibitors*
  • Tetrazoles / pharmacology
  • Thrombosis / chemically induced
  • Thrombosis / prevention & control*
  • Time Factors

Substances

  • Chlorides
  • Ferric Compounds
  • Fibrinolytic Agents
  • Indans
  • Platelet Aggregation Inhibitors
  • Receptors, Thromboxane
  • Tetrazoles
  • Z 335
  • Cilostazol
  • ferric chloride