NF279: a novel potent and selective antagonist of P2X receptor-mediated responses

Eur J Pharmacol. 1998 May 29;350(1):R5-6. doi: 10.1016/s0014-2999(98)00316-1.

Abstract

8,8'-(Carbonylbis(imino-4, 1 -phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis(1,3, 5-naphthalenetrisulfonic acid) (NF279) antagonized P2X receptor-mediated contractions in rat vas deferens, evoked by alpha,beta-methylene ATP (10 microM; pIC50=5.71) without affecting responses mediated via alpha1A-adrenoceptors, adenosine A1 and A2B receptors, histamine H1, muscarinic M3 and nicotinic receptors. The low inhibitory potency of NF279 on P2Y receptors in guinea-pig taenia coli (pA2=4.10) and at ecto-nucleotidases in folliculated Xenopus laevis oocytes (IC50 > 100 microM) indicates that NF279 is a novel specific and selective P2X receptor antagonist.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Animals
  • Colon / drug effects
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Oocytes / drug effects
  • Purinergic P2 Receptor Antagonists*
  • Rats
  • Suramin / analogs & derivatives*
  • Suramin / pharmacology
  • Vas Deferens / drug effects
  • Vasoconstriction / drug effects
  • Xenopus laevis

Substances

  • NF 279
  • Purinergic P2 Receptor Antagonists
  • Suramin
  • Adenosine Triphosphate