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NF279: a novel potent and selective antagonist of P2X receptor-mediated responses
- 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.
- Subjects :
- Male
medicine.medical_specialty
P2Y receptor
medicine.drug_class
Colon
Guinea Pigs
Suramin
Biology
In Vitro Techniques
chemistry.chemical_compound
Xenopus laevis
Adenosine Triphosphate
Vas Deferens
Internal medicine
Muscarinic acetylcholine receptor
medicine
Purinergic P2 Receptor Antagonists
Animals
Receptor
Pharmacology
Antagonist
Taenia coli
Receptor antagonist
Adenosine
Rats
Endocrinology
medicine.anatomical_structure
chemistry
Vasoconstriction
Oocytes
Histamine
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 350
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- European journal of pharmacology
- Accession number :
- edsair.doi.dedup.....162a70e76a79bcf952c24afb686c7d00