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 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.
Department of Pharmacology, Biocentre Niederursel, University of Frankfurt, Frankfurt/M., Germany.
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S
Damer
B
B
Niebel
S
S
Czeche
P
P
Nickel
U
U
Ardanuy
G
G
Schmalzing
J
J
Rettinger
E
E
Mutschler
G
G
Lambrecht
D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D003106:Colon / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009865:Oocytes / Q000187:drug effects; D058919:Purinergic P2 Receptor Antagonists; D051381:Rats; D013498:Suramin / Q000031:analogs & derivatives* / Q000494:pharmacology; D014649:Vas Deferens / Q000187:drug effects; D014661:Vasoconstriction / Q000187:drug effects; D014982:Xenopus laevis
C114657:NF 279; D058919:Purinergic P2 Receptor Antagonists; D013498:Suramin; D000255:Adenosine Triphosphate