N-Substituted analogues of S-nitroso-N-acetyl-D,L-penicillamine: chemical stability and prolonged nitric oxide mediated vasodilatation in isolated rat femoral arteries

Br J Pharmacol. 1999 Feb;126(3):639-48. doi: 10.1038/sj.bjp.0702346.

Abstract

Previous studies show that linking acetylated glucosamine to S-nitroso-N-acetyl-D,L-penicillamine (SNAP) stabilizes the molecule and causes it to elicit unusually prolonged vasodilator effects in endothelium-denuded, isolated rat femoral arteries. Here we studied the propanoyl (SNPP; 3 carbon side-chain), valeryl (SNVP; 5C) and heptanoyl (SNHP; 7C) N-substituted analogues of SNAP (2C), to further investigate other molecular characteristics that might influence chemical stability and duration of vascular action of S-nitrosothiols. Spectrophotometric analysis revealed that SNVP was the most stable analogue in solution. Decomposition of all four compounds was accelerated by Cu(II) and cysteine, and neocuproine, a specific Cu(I) chelator, slowed decomposition of SNHP. Generation of NO from the compounds was confirmed by electrochemical detection at 37 degrees C. Bolus injections of SNAP (10 microl; 10(-8)-10(-3) M) into the perfusate of precontracted, isolated rat femoral arteries taken from adult male Wistar rats (400-500 g), caused concentration-dependent, transient vasodilatations irrespective of endothelial integrity. Equivalent vasodilatations induced by SNVP and SNHP were transient in endothelium-intact vessels but failed to recover to pre-injection pressures at moderate and high concentrations (10(-6)-10(-3) M) in those denuded of endothelium. This sustained effect (> 1 h) was most prevalent with SNHP and was largely reversed by the NO scavenger, haemoglobin. We suggest that increased lipophilicity of SNAP analogues with longer sidechains facilitates their retention by endothelium-denuded vessels; subsequent slow decomposition within the tissue generates sufficient NO to cause prolonged vasodilatation. This is a potentially useful characteristic for targeting NO delivery to areas of endothelial damage.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Octanol
  • Animals
  • Endothelium, Vascular / physiology
  • Femoral Artery / drug effects
  • Femoral Artery / physiology
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Male
  • Nitric Oxide / metabolism
  • Nitric Oxide / physiology
  • Nitric Oxide Donors / pharmacology
  • Penicillamine / analogs & derivatives*
  • Penicillamine / chemistry
  • Penicillamine / metabolism
  • Penicillamine / pharmacology
  • Rats
  • Rats, Wistar
  • Solubility
  • Vasodilation / drug effects
  • Water

Substances

  • Nitric Oxide Donors
  • S-nitro-N-acetylpenicillamine
  • Water
  • Nitric Oxide
  • Penicillamine
  • 1-Octanol