Vasorelaxant and platelet-suppressant potencies of four NO-donors

Pol J Pharmacol Pharm. 1990 May-Jun;42(3):275-81.

Abstract

Rabbit aortic strips were arranged in a Vane's cascade and superfused with Krebs buffer which contained phenylephrine hydrochloride (100 nM) and indomethacin (5 microM). EC50 (nM) for vasorelaxant action of NO-donors on rabbit aortic strips were as follows: glyceryl trinitrate--64.0, sodium nitroprusside--124.5, S-nitroso-N-acetylpenicillamine--305.7, SIN-1 (metabolite of molsidomine)--510.0. On the other hand IC50 (microM) for antiaggregatory action of NO-donors in human platelet rich plasma aggregated with threshold concentrations of collagen (0.5-1 micrograms/ml) were as follows: S-nitroso-N-acetylpenicillamine--7,1, SIN-1--13.6, sodium nitroprusside--28.0. Glyceryl trinitrate did not inhibit platelet aggregation at concentrations up to 1 mM. Sodium nitroprusside was more specific (EC50/IC50 = 0.0043) than SNAP and SIN-1 (EC50/IC50 = 0.043 and 0.037, respectively) as a vasorelaxant than as a platelet suppressant. Thus relative potencies of four c-GMP stimulants as vasorelaxants and platelet-suppressants differed considerably and several possible explanations for these differences were put forward.

MeSH terms

  • Animals
  • Aorta / drug effects
  • Humans
  • In Vitro Techniques
  • Molsidomine / analogs & derivatives
  • Molsidomine / pharmacology
  • Nitric Oxide / metabolism*
  • Nitroglycerin / pharmacology
  • Nitroprusside / pharmacology
  • Penicillamine / analogs & derivatives
  • Penicillamine / pharmacology
  • Platelet Aggregation Inhibitors*
  • Rabbits
  • S-Nitroso-N-Acetylpenicillamine
  • Vasodilator Agents*

Substances

  • Platelet Aggregation Inhibitors
  • Vasodilator Agents
  • Nitroprusside
  • Nitric Oxide
  • linsidomine
  • S-Nitroso-N-Acetylpenicillamine
  • Molsidomine
  • Nitroglycerin
  • Penicillamine