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

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 mu M; PIC50 = 5.71) without affecting responses mediated via alpha(1A)-adrenoceptors, adenosine A(1) and A(2B) receptors, histamine H-1, muscarinic M-3 and nicotinic receptors. The low inhibitory potency of NF279 on P2Y receptors in guinea-pig taenia coli (pA(2) = 4.10) and at ecto-nucleotidases in folliculated Xenopus laevis oocytes (IC50 > 100 mu M) indicates that NF279 is a novel specific and selective P2X receptor antagonist. (C) 1998 Elsevier Science B.V. All rights reserved.