ArticleBritish journal of pharmacology1996
Inhibition of ecto-ATPase by PPADS, suramin and reactive blue in endothelial cells, C6 glioma cells and RAW 264.7 macrophages.
Article in British journal of pharmacology, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 94 citations in OpenAlex.
- Nucleotide-Derived Competitive Inhibitors of Ectonucleotidase CD39─A Promising Extracellular Target for Immunotherapy of Cancer.Journal of medicinal chemistry · 2026Article
- The real-time detection of acupuncture-induced extracellular ATP mobilization in acupoints and exploration of its role in acupuncture analgesia.Purinergic signalling · 2023Article
- Stimulation-induced increases in cerebral blood flow and local capillary vasoconstriction depend on conducted vascular responses.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- The role of ATP signalling in response to mechanical stimulation studied in T24 cells using new microphysiological tools.Journal of cellular and molecular medicine · 2018Article
- UDP-sugars activate P2YVascular pharmacology · 2018Article
- POM-1 inhibits P2 receptors and exhibits anti-inflammatory effects in macrophages.Purinergic signalling · 2017Article
- ATP release during cell swelling activates a CaScientific reports · 2017Article
- The effect of purinergic P2 receptor blockade on skeletal muscle exercise hyperemia in miniature swine.European journal of applied physiology · 2014Article
- Ticlopidine in its prodrug form is a selective inhibitor of human NTPDase1.Mediators of inflammation · 2014Article
- 8-BuS-ATP derivatives as specific NTPDase1 inhibitors.British journal of pharmacology · 2013Article
- Ecto-nucleoside triphosphate diphosphohydrolase 2 modulates local ATP-induced calcium signaling in human HaCaT keratinocytes.PloS one · 2013Article
- Modulation of ATP-induced LTP by cannabinoid receptors in rat hippocampus.Purinergic signalling · 2012Article
- Metabolism of circulating ADP in the bloodstream is mediated via integrated actions of soluble adenylate kinase-1 and NTPDase1/CD39 activities.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
- Contribution of renal purinergic receptors to renal vasoconstriction in angiotensin II-induced hypertensive rats.American journal of physiology. Renal physiology · 2011Article
- P2X(1) receptor blockade inhibits whole kidney autoregulation of renal blood flow in vivo.American journal of physiology. Renal physiology · 2010Article
- Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases).Purinergic signalling · 2009Article
- Mechanism of ATP-induced local and conducted vasomotor responses in isolated rat cerebral penetrating arterioles.Journal of vascular research · 2009Article
- Selective nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5'-carboxamide.Journal of medicinal chemistry · 2008Article
- A capillary electrophoresis method for the characterization of ecto-nucleoside triphosphate diphosphohydrolases (NTPDases) and the analysis of inhibitors by in-capillary enzymatic microreaction.Purinergic signalling · 2005Article
- Multiple P2Y receptors couple to calcium-dependent, chloride channels in smooth muscle cells of the rat pulmonary artery.Respiratory research · 2005Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
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Abstract
1. Previous studies have shown that bovine pulmonary artery endothelium (CPAE) has P2Y and P2U purinoceptors, rat C6 glioma cells have P2U purinoceptors and mouse RAW 264.7 cells have pyrimidinoceptors, all of which are coupled to phosphoinositide-specific phospholipase C (PI-PLC). The dual actions of PPADS, suramin and reactive blue as antagonists of receptor subtypes and ecto-ATPase inhibitors were studied in these three cell types. 2. In CPAE, suramin, at 3-100 microM, competitively inhibited the PI responses induced by 2MeSATP and UTP, with pA2 values of 5.5 +/- 0.3 and 4.4 +/- 0.4, respectively. Reactive blue, at 1-3 microM, produced shifts to the right of the 2MeSATP and UTP curves, but no further right shift at 10 microM. PPADS, at 10 microM, caused a 3 fold right shift of the 2MeSATP curve, but no further shift at concentrations up to 100 microM. In contrast, a dose-dependent shift to the left of the UTP curve and a weak inhibition of the ATP response were seen with PPADS. 3. In RAW 264.7 cells, suramin and reactive blue, but not PPADS, competitively inhibited the UTP response, with pA2 values of 4.8 +/- 0.5 and 5.8 +/- 0.7, respectively. 4. In C6 glioma cells, although suramin and reactive blue inhibited the ATP response, a potentiation effect on ATP and UTP responses was seen with PPADS. 5. The ecto-ATPase inhibitory activity of these three receptor antagonists were determined. All three inhibited ecto-ATPase present in CPAE, C6 and RAW 264.7 cells, with IC50 values of 4, 4.8 and 4.7 for PPADS, 4, 4.4 and > > 4 for suramin, and 4.5, 4.7 and 4.7 for reactive blue. 6. This study indicates that PPADS, suramin and reactive blue ar ecto-ATPase inhibitors. This property, combined with their antagonistic selectivity for receptor subtypes, can result in inhibition of, potentiation of, or lack of effect on agonist-mediated PI responses. Reactive blue is a more potent antagonist than suramin on P2Y, P2U and pyrimidinoceptors, and PPADS is a weak antagonist for P2Y receptors.
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