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2,4'-Nitrophenylisatogen potentiates P2X1 receptor mediated vascular contraction and blood pressure elevation.
Department of Cardiology, Lund University, Lund, Sweden.
Organic Chemistry, Novum, Karolinska Institute, Stockholm, Sweden.ORCID iD: 0000-0002-8444-181X
Clinical Pharmacology, Gothenburg University, Gothenburg, Sweden.
Clinical Pharmacology, Gothenburg University, Gothenburg, Sweden.
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2003 (English)In: Drug development research (Print), ISSN 0272-4391, E-ISSN 1098-2299, Vol. 59, no 1, 82-87 p.Article in journal (Refereed) Published
Abstract [en]

The objective of this research was to examine the effects of chem. compds. with possible P2 receptor modulating effects and to characterize the potentiating effects of 2,4'-nitrophenylisatogen (NPI) on P2X1 receptors in vitro and in vivo. Chem. compds. were tested in an in vitro pharmacol. assay using vascular segments from the rat mesenteric artery stimulated by P2 receptor-specific agonists. Contractions were expressed as a percentage of 60 mM K+-induced contractions. Blood pressure was evaluated in pithed rats. NPI (30 ΌM) added 15 min before addn. of the P2X1 receptor-specific agonist αβ-MeATP increased the max. vasoconstriction from 23% to 49% (an increase of 113%). Furthermore, NPI prevented the desensitization of repeated αβ-MeATP contractions. Related compds. were examd., and 2-(3-methoxy-phenyl)-1-oxy-indol-3-one (MPI) had similar effects as NPI, but several others lacked effect. NPI had no effect on ADPβS (P2Y1) or acetylcholine-mediated vasodilatation, nor on UTP (P2Y2/4), UDP (P2Y6), or noradrenaline-mediated contractions. In pithed rats, the blood pressure response to 50 nmol/kg-infusion of αβ-MeATP was increased from 50 to 63 mmHg, but had no effect on basal blood pressure or on the cardiovascular response to preganglionic nerve stimulation. In conclusion, NPI and MPI potentiates P2X1 receptor vascular contractions in vitro and (NPI) blood pressure effects in vivo. It is possible that the effect is mediated by an inhibition of P2X1 receptor desensitization. [on SciFinder(R)]

Place, publisher, year, edition, pages
2003. Vol. 59, no 1, 82-87 p.
Keyword [en]
nitrophenylisatogen purinergic P2X1 receptor vasoconstriction blood pressure, structure nitrophenylisatogen analog purinergic P2X1 receptor antagonist
National Category
Organic Chemistry
URN: urn:nbn:se:kth:diva-92002DOI: 10.1002/ddr.10205OAI: diva2:511787
CAPLUS AN 2003:468824(Journal) NR 20140805Available from: 2012-03-23 Created: 2012-03-23 Last updated: 2012-03-23Bibliographically approved

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Slätt, Johnny
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