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

S Damer, B Niebel, S Czeche, P Nickel… - European journal of …, 1998 - Elsevier
S Damer, B Niebel, S Czeche, P Nickel, U Ardanuy, G Schmalzing, J Rettinger, E Mutschler…
European journal of pharmacology, 1998Elsevier
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 α, β-methylene ATP (10 μM; pIC50= 5.71)
without affecting responses mediated via α1A-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 …
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 α,β-methylene ATP (10 μM; pIC50=5.71) without affecting responses mediated via α1A-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 μM) indicates that NF279 is a novel specific and selective P2X receptor antagonist.
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