Pharmacological profile of G619, a new platelet aggregation inhibitor

Thromb Res. 1992 May 15;66(4):331-47. doi: 10.1016/0049-3848(92)90283-g.

Abstract

G619, a 4-OH-isophthalic acid derivative, was studied for its capacity to inhibit platelet aggregation. G619 dose-dependently inhibited U46619, collagen, ADP, PAF, thrombin and epinephrine-induced platelet aggregation in vitro. The IC50 values for inhibition of U46619-induced human and rabbit platelet aggregation were 39 and 43 microM, respectively. G619, at 100 microM, inhibited high concentration collagen (10 micrograms/ml)-induced aggregation of rabbit platelets pretreated with indomethacin and increased the level of cAMP in washed rabbit platelets by 30% (p less than 0.01 vs basal). However, G619, did not inhibit fibrinogen binding to GPIIb/IIIa receptor, phosphodiesterase, U46619-induced contractile responses on canine saphenous vein or rabbit aorta, calcium-induced vasoconstriction and thrombin or PAF-induced elevation of [Ca++]i in platelets in vitro. In vivo, the U46619-induced maximal thrombocytopenia in rats was reduced from 40% (vehicle) to 22% and 18% by 10 and 30 mg/kg of G619 i.v., respectively. G619 (30 mg/kg) had no effect on the U46619-induced vasopressor response or sudden death in rats, and had no effect on TxB2 formation. Our results indicate that G619 is a broad-spectrum platelet aggregation inhibitor and may have its effect on a common mechanism for platelet aggregation besides an effect on the thromboxane A2 receptor.

MeSH terms

  • Adenosine Diphosphate / antagonists & inhibitors
  • Animals
  • Benzamides / pharmacology*
  • Calcium / pharmacology
  • Collagen / antagonists & inhibitors
  • Dogs
  • Epinephrine / antagonists & inhibitors
  • Fibrinogen / metabolism
  • Humans
  • Male
  • Phenylacetates / pharmacology
  • Picolines / pharmacology*
  • Platelet Activating Factor / antagonists & inhibitors
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Membrane Glycoproteins / drug effects
  • Platelet Membrane Glycoproteins / metabolism
  • Prostaglandin Endoperoxides, Synthetic / antagonists & inhibitors
  • Prostaglandin Endoperoxides, Synthetic / toxicity
  • Rabbits
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Thromboxane / antagonists & inhibitors*
  • Shock, Septic / blood
  • Sulfonamides / pharmacology
  • Thrombin / antagonists & inhibitors
  • Thromboxane B2 / biosynthesis
  • Vasoconstriction / drug effects

Substances

  • Benzamides
  • Phenylacetates
  • Picolines
  • Platelet Activating Factor
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Prostaglandin Endoperoxides, Synthetic
  • Receptors, Thromboxane
  • Sulfonamides
  • 3-carbamyl-(3'-picolyl)-4-methoxy-1-benzamide
  • Thromboxane B2
  • Adenosine Diphosphate
  • Fibrinogen
  • Collagen
  • Thrombin
  • daltroban
  • Calcium
  • Epinephrine