The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors

Eur J Pharmacol. 2000 Jan 17;387(3):R19-21. doi: 10.1016/s0014-2999(99)00834-1.

Abstract

Pyridoxal-5'-phosphate-6-(2'-naphthylazo-6'-nitro-4',8'-disulfonat e) (PPNDS) potently antagonized P2X(1) receptor-mediated responses in rat vas deferens (pK(B)=7.43) and Xenopus laevis oocytes (pIC(50)=7. 84). It showed lower (up to 20,000-fold) inhibitory potency on ecto-nucleotidase in Xenopus oocytes and on P2Y(1) receptors in guinea-pig ileum (pA(2)=6.13). PPNDS did not interact with alpha(1A)-adrenoceptors, adenosine A(1) and A(2B), histamine H(1) and muscarinic M(3) receptors. Thus, PPNDS is a novel, specific P2 receptor antagonist and represents the pyridoxal-5'-phosphate derivative with the highest potency at P2X(1) receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Purinergic P2 Receptor Antagonists*
  • Pyridoxal Phosphate / analogs & derivatives*
  • Pyridoxal Phosphate / pharmacology
  • Rats
  • Sulfonic Acids / pharmacology*
  • Xenopus

Substances

  • Purinergic P2 Receptor Antagonists
  • Sulfonic Acids
  • pyridoxal-5'-phosphate-6-(2'-naphthylazo-6'-nitro-4',8'-disulfonate)
  • pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
  • Pyridoxal Phosphate