Novel S-nitrosothiols do not engender vascular tolerance and remain effective in glyceryl trinitrate-tolerant rat femoral arteries

Eur J Pharmacol. 2000 Sep 1;403(1-2):111-9. doi: 10.1016/s0014-2999(00)00572-0.

Abstract

Organic nitrates, such as glyceryl trinitrate, are nitric oxide (NO) donor drugs that engender tolerance with long-term use. Here, we tested the hypothesis that our novel S-nitrosothiols, N-(S-nitroso-N-acetylpenicillamine)-2-amino-2-deoxy-1,3,4,6, tetra-O-acetyl-beta-D-glucopyranose (RIG200) and S-nitroso-N-valeryl-D-penicillamine (D-SNVP), do not induce vascular tolerance ex vivo. Femoral arteries from adult male Wistar rats were preconstricted with phenylephrine and perfused with the NO synthase inhibitor N(omega)-nitro-L-arginine methyl ester (L-NAME). Perfusion pressure was measured during 20-h treatment with supramaximal concentrations of NO donor (10 microM). Perfusion with glyceryltrinitrate caused a vasodilatation, which recovered over 2-20 h. In contrast, the S-nitrosothiols caused vasodilatations that were maintained throughout the 20-h perfusion period. Responses to S-nitrosothiols were partially reversed by the NO scavenger ferrohaemoglobin and fully reversed by the soluble guanylate cyclase inhibitor [1H-[1,2,4] oxadiazole [4,3-a]quinoxaline-1-one (ODQ). Glyceryltrinitrate-tolerant vessels were fully responsive to bolus injections of S-nitrosothiols. Resistance to tolerance is an attractive property of our novel compounds, particularly in view of their sustained activity in arteries with damaged endothelium.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Drug Tolerance
  • Enzyme Inhibitors / pharmacology
  • Femoral Artery / drug effects*
  • Femoral Artery / physiology
  • Glucosamine / analogs & derivatives*
  • Glucosamine / pharmacology*
  • Glutathione / analogs & derivatives*
  • Hemoglobins / pharmacology
  • In Vitro Techniques
  • NG-Nitroarginine Methyl Ester / pharmacology
  • Nitric Oxide Donors / pharmacology
  • Nitroglycerin / pharmacology*
  • Nitroso Compounds / pharmacology
  • Oxadiazoles / pharmacology
  • Penicillamine / analogs & derivatives*
  • Penicillamine / pharmacology*
  • Perfusion
  • Phenylephrine / pharmacology
  • Quinoxalines / pharmacology
  • Rats
  • Rats, Wistar
  • S-Nitrosoglutathione
  • Vasoconstriction / drug effects
  • Vasoconstrictor Agents / pharmacology
  • Vasodilator Agents / pharmacology*

Substances

  • 1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
  • Enzyme Inhibitors
  • Hemoglobins
  • Nitric Oxide Donors
  • Nitroso Compounds
  • Oxadiazoles
  • Quinoxalines
  • RIG 200
  • Vasoconstrictor Agents
  • Vasodilator Agents
  • Phenylephrine
  • S-Nitrosoglutathione
  • S-nitrosopenicillamine
  • Nitroglycerin
  • Glutathione
  • Penicillamine
  • Glucosamine
  • NG-Nitroarginine Methyl Ester