ArticleBritish journal of pharmacology1999
Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 100 citations in OpenAlex.
- Diadenosine pentaphosphate regulates dendrite growth and number in cultured hippocampal neurons.Purinergic signalling · 2024Article
- The P2X1 receptor as a therapeutic target.Purinergic signalling · 2022Review
- Heteromeric assembly of P2X subunits.Frontiers in cellular neuroscience · 2013Review
- The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.British journal of pharmacology · 2013Article
- ATP binding site mutagenesis reveals different subunit stoichiometry of functional P2X2/3 and P2X2/6 receptors.The Journal of biological chemistry · 2012Article
- Purinergic modulation of granule cells.Cerebellum (London, England) · 2012Review
- Activation and regulation of purinergic P2X receptor channels.Pharmacological reviews · 2011Review
- Pharmacochemistry of the platelet purinergic receptors.Purinergic signalling · 2011Article
- Uridine adenosine tetraphosphate-induced contraction is increased in renal but not pulmonary arteries from DOCA-salt hypertensive rats.American journal of physiology. Heart and circulatory physiology · 2011Article
- P2X(1) receptor blockade inhibits whole kidney autoregulation of renal blood flow in vivo.American journal of physiology. Renal physiology · 2010Article
- Dinucleoside polyphosphates: strong endogenous agonists of the purinergic system.British journal of pharmacology · 2009Review
- Uridine adenosine tetraphosphate acts as an autocrine hormone affecting glomerular filtration rate.Journal of molecular medicine (Berlin, Germany) · 2008Article
- P2X3 receptor involvement in pain states.Molecular neurobiology · 2007Review
- Pharmacology of P2X channels.Pflugers Archiv : European journal of physiology · 2006Review
- P2X2 knockout mice and P2X2/P2X3 double knockout mice reveal a role for the P2X2 receptor subunit in mediating multiple sensory effects of ATP.The Journal of physiology · 2005Article
- Antagonism of ATP responses at P2X receptor subtypes by the pH indicator dye, Phenol red.British journal of pharmacology · 2005Article
- Molecular recognition at adenine nucleotide (P2) receptors in platelets.Seminars in thrombosis and hemostasis · 2005Review
- Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats.British journal of pharmacology · 2004Article
- Molecular recognition at purine and pyrimidine nucleotide (P2) receptors.Current topics in medicinal chemistry · 2004Review
- Purine and pyrimidine (P2) receptors as drug targets.Journal of medicinal chemistry · 2002Review
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The antagonist activity of a series of diinosine polyphosphates (IpnI, where n=3, 4, 5) was assessed against ATP-activated inward currents at rat P2X(1-4) receptors expressed in Xenopus oocytes and studied under voltage-clamp conditions. 2. Diinosine polyphosphates were prepared by the enzymatic degradation of their corresponding diadenosine polyphosphates (e.g., Ap5A into Ip5I) using 5'-adenylic deaminase, and purified using reverse-phase chromatography. 3. Against ATP-responses at rP2X1 receptors, the potency order for antagonism was (pIC50): Ip5I (8.5)>Ip4I (6.3)>Ip3I (>4.5). Ip5I (10-100 nM) caused a concentration-dependent rightwards displacement of the ATP concentration-response curve without reducing the maximum ATP effect. However, the Schild plot was non-linear which indicated Ip5I is not a competitive antagonist. Blockade by micromolar concentrations of Ip5I was not surmountable. Ip4I also behaved as a non-surmountable antagonist. 4. Against ATP-responses at rP2X3 receptors, the potency order for antagonism was (pIC50): Ip4I (6. 0)>Ip5I (5.6)>Ip3I (>4.5). Blockade by Ip4I (pA2, 6.75) and Ip5I (pA2, 6.27) was surmountable at micromolar concentrations. 5. Diinosine polyphosphates failed to inhibit ATP-responses at rP2X2 receptors, whereas agonist responses at rP2X4 were reversibly potentiated by Ip4I and Ip5I. None of the parent diadenosine polyphosphates behave as antagonists at rP2X1 - 4 receptors. 6. Thus, Ip5I acted as a potent and relatively-selective antagonist at the rP2X1 receptor. This dinucleotide pentaphosphate represents a high-affinity antagonist for the P2X1 receptor, at which it acts in a competitive manner at low (</=100 nM) concentrations but has more complex actions at higher (>100 nM) concentrations.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.