ArticleBritish journal of pharmacology2002
Kinetics of antagonist actions at rat P2X2/3 heteromeric receptors.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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23 citing papers in PubMed, 54 citations in OpenAlex.
- Subtype-Specific Ligand Binding and Activation Gating in Homomeric and Heteromeric P2X Receptors.Biomolecules · 2024Article
- DT-0111: a novel P2X3 receptor antagonist.Purinergic signalling · 2023Article
- Diclofenac and other non-steroidal anti-inflammatory drugs (NSAIDs) are competitive antagonists of the human P2X3 receptor.Frontiers in pharmacology · 2023Article
- Enlightening activation gating in P2X receptors.Purinergic signalling · 2022Review
- Action of MK-7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation.British journal of pharmacology · 2019Article
- Small organic molecule disruptors of Cav3.2 - USP5 interactions reverse inflammatory and neuropathic pain.Molecular pain · 2015Article
- Comparative analysis of P2X1, P2X2, P2X3, and P2X4 receptor subunits in rat nodose ganglion neurons.PloS one · 2014Article
- Heteromeric assembly of P2X subunits.Frontiers in cellular neuroscience · 2013Review
- Article
- Activation and regulation of purinergic P2X receptor channels.Pharmacological reviews · 2011Review
- A residue in the TRPM2 channel outer pore is crucial in determining species-dependent sensitivity to extracellular acidic pH.Pflugers Archiv : European journal of physiology · 2011Article
- Identification of P2X₃ and P2X₇ purinergic receptors activated by ATP in rat lacrimal gland.Investigative ophthalmology & visual science · 2011Article
- State-dependent inhibition of TRPM2 channel by acidic pH.The Journal of biological chemistry · 2010Article
- Purinergic mechanosensory transduction and visceral pain.Molecular pain · 2009Review
- Pharmacology of P2X channels.Pflugers Archiv : European journal of physiology · 2006Review
- Methyllycaconitine, alpha-bungarotoxin and (+)-tubocurarine block fast ATP-gated currents in rat dorsal root ganglion cells.British journal of pharmacology · 2004Article
- P2X3 receptors and peripheral pain mechanisms.The Journal of physiology · 2004Review
- Molecular recognition at purine and pyrimidine nucleotide (P2) receptors.Current topics in medicinal chemistry · 2004Review
- ATP analogues with modified phosphate chains and their selectivity for rat P2X2 and P2X2/3 receptors.British journal of pharmacology · 2003Article
- Dehydroepiandrosterone potentiates native ionotropic ATP receptors containing the P2X2 subunit in rat sensory neurones.The Journal of physiology · 2003Article
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4 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
1. Currents through heteromeric P2X(2/3) receptors were evoked by applying alpha,beta-methylene-ATP to human embryonic kidney cells transfected with cDNAs encoding the P2X(2) and P2X(3) subunits. The concentration of alpha,beta-methylene-ATP were < or =30 microM because higher concentrations can activate homomeric P2X(2) receptors. The kinetics of action of three structurally unrelated antagonists were studied; these were 2', 3'-O-(2,4,6,trinitrophenyl)-ATP (TNP-ATP), pyridoxal-5-phosphate-6-azophenyl-2',4'-disulphonate (PPADS) and suramin. The association and dissociation rate constants were determined by pre-applying the antagonist for various periods prior to the co-application of agonist and antagonist, or by changing the solution from one containing only the agonist to one containing both agonist and antagonist. The high affinity of TNP-ATP for the P2X(2/3) receptor (K(D) approximately 2 nM) results from fast binding (k(+1) approximately 100 microM(-1) s(-1)) rather than slow unbinding (k(-1) approximately 0.3 s(-1)). For suramin (K(D) approximately 1 microM) the association rate constant ( approximately 1 microM(-1) s(-1)) was 100 times slower than that of TNP-ATP but the dissociation rate constant was similar (k(-1) approximately 1 s(-1)). PPADS (K(D) approximately 0.1 microM) associated and dissociated some 100 - 10,000 times more slowly than the other antagonists.
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