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

Authors :
Peter Nickel
Ernst Mutschler
Günter Lambrecht
Beate Niebel
Jürgen Rettinger
Ursula Ardanuy
Sittah Czeche
Günther Schmalzing
Susanne Damer
Source :
European journal of pharmacology. 350(1)
Publication Year :
1998

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.

Details

ISSN :
00142999
Volume :
350
Issue :
1
Database :
OpenAIRE
Journal :
European journal of pharmacology
Accession number :
edsair.doi.dedup.....162a70e76a79bcf952c24afb686c7d00