AH23848: a thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A2

Circulation. 1985 Dec;72(6):1208-18. doi: 10.1161/01.cir.72.6.1208.

Abstract

Despite numerous suggestions in the literature that thromboxane A2 is involved in a variety of occlusive vascular diseases, no definitive evidence is available. Arguments have been presented to support the view that such evidence can only come from clinical studies with a highly specific thromboxane receptor-blocking drug. We have now identified such a drug, AH23848, in our laboratories. Preliminary experiments with AH23848, ([1 alpha (Z), 2 beta,5 alpha]-(+/-)-7-[5-[[(1,1'-biphenyl)-4-yl]methoxy]-2-(4-morpholin yl)-3-oxocyclopentyl]-4-heptenoic acid), show that it is a potent, specific thromboxane receptor-blocking drug that is orally active and has a long duration of action. It should be a valuable tool in elucidating any physiologic or pathologic role of thromboxane A2.

MeSH terms

  • Angina Pectoris / drug therapy
  • Animals
  • Biphenyl Compounds / pharmacology*
  • Biphenyl Compounds / therapeutic use
  • Collagen / pharmacology
  • Dogs
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • Humans
  • In Vitro Techniques
  • Male
  • Muscle, Smooth, Vascular / drug effects
  • Platelet Aggregation / drug effects
  • Rats
  • Receptors, Cell Surface / drug effects*
  • Receptors, Prostaglandin / drug effects*
  • Receptors, Thromboxane
  • Shock, Septic / drug therapy
  • Thromboxane A2 / physiology*
  • Thromboxane-A Synthase / antagonists & inhibitors
  • Vasoconstriction / drug effects

Substances

  • Biphenyl Compounds
  • Receptors, Cell Surface
  • Receptors, Prostaglandin
  • Receptors, Thromboxane
  • Thromboxane A2
  • AH 23848
  • Collagen
  • Thromboxane-A Synthase