Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Diinosine pentaphosphate: an antagonist which discriminates between recombinant P2X(3) and P2X(2/3) receptors and between two P2X receptors in rat sensory neurones.
???displayArticle.abstract???
1. We have compared the antagonist activity of trinitrophenyl-ATP (TNP-ATP) and diinosine pentaphosphate (Ip(5)I) on recombinant P2X receptors expressed in Xenopus oocytes with their actions at native P2X receptors in sensory neurones from dorsal root and nodose ganglia. 2. Slowly-desensitizing responses to alpha,beta-methylene ATP (alpha,beta-meATP) recorded from oocytes expressing P2X(2/3) receptors were inhibited by TNP-ATP at sub-micromolar concentrations. However, Ip(5)I at concentrations up to 30 microM was without effect. 3. Nodose ganglion neurones responded to alpha,beta-meATP with slowly-desensitizing inward currents. These were inhibited by TNP-ATP (IC(50), 20 nM), but not by Ip(5)I at concentrations up to 30 microM. 4. In DRG neurones that responded to ATP with a rapidly-desensitizing inward current, the response was inhibited by TNP-ATP with an IC(50) of 0.8 nM. These responses were also inhibited by Ip(5)I with an IC(50) of 0.1 microM. Both antagonists are known to inhibit homomeric P2X(3) receptors. 5. Some DRG neurones responded to alpha,beta-meATP with a biphasic inward current, consisting of transient and sustained components. While the transient current was abolished by 1 microM Ip(5)I, the sustained component remained unaffected. 6. In conclusion, Ip(5)I is a potent antagonist at homomeric P2X(3) receptors but not at heteromeric P2X(2/3) receptors, and therefore should be a useful tool for elucidating the subunit composition of native P2X receptors.
Burgard,
P2X receptor-mediated ionic currents in dorsal root ganglion neurons.
1999,
Pubmed Burnstock,
Purinergic receptors: their role in nociception and primary afferent neurotransmission.
1996,
Pubmed Burnstock,
P2X receptors in sensory neurones.
2000,
Pubmed Chen,
A P2X purinoceptor expressed by a subset of sensory neurons.
1995,
Pubmed
,
Xenbase Collo,
Cloning OF P2X5 and P2X6 receptors and the distribution and properties of an extended family of ATP-gated ion channels.
1996,
Pubmed Cook,
Distinct ATP receptors on pain-sensing and stretch-sensing neurons.
1997,
Pubmed Ding,
Inactivation of P2X2 purinoceptors by divalent cations.
2000,
Pubmed Dunn,
Discrimination between subtypes of apamin-sensitive Ca(2+)-activated K+ channels by gallamine and a novel bis-quaternary quinolinium cyclophane, UCL 1530.
1996,
Pubmed Evans,
Pharmacological characterization of heterologously expressed ATP-gated cation channels (P2x purinoceptors).
1995,
Pubmed Grubb,
Characterization of cultured dorsal root ganglion neuron P2X receptors.
1999,
Pubmed Jahr,
ATP excites a subpopulation of rat dorsal horn neurones.
,
Pubmed Khakh,
Electrophysiological properties of P2X-purinoceptors in rat superior cervical, nodose and guinea-pig coeliac neurones.
1995,
Pubmed Kim,
Molecular assembly of the extracellular domain of P2X2, an ATP-gated ion channel.
1997,
Pubmed King,
Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors.
1999,
Pubmed
,
Xenbase King,
Effects of extracellular pH on agonism and antagonism at a recombinant P2X2 receptor.
1997,
Pubmed
,
Xenbase King,
A role for calcineurin in the desensitization of the P2X3 receptor.
1997,
Pubmed
,
Xenbase Kirkup,
Excitatory effect of P2X receptor activation on mesenteric afferent nerves in the anaesthetised rat.
1999,
Pubmed Krishtal,
Receptor for ATP in the membrane of mammalian sensory neurones.
1983,
Pubmed Lewis,
The ion channel properties of a rat recombinant neuronal nicotinic receptor are dependent on the host cell type.
1997,
Pubmed
,
Xenbase Lewis,
Coexpression of P2X2 and P2X3 receptor subunits can account for ATP-gated currents in sensory neurons.
1995,
Pubmed Nicke,
P2X1 and P2X3 receptors form stable trimers: a novel structural motif of ligand-gated ion channels.
1998,
Pubmed
,
Xenbase Robertson,
Characterization of a P2X-purinoceptor in cultured neurones of the rat dorsal root ganglia.
1996,
Pubmed Rong,
P2X purinoceptor-mediated excitation of trigeminal lingual nerve terminals in an in vitro intra-arterially perfused rat tongue preparation.
2000,
Pubmed Smith,
Identification of amino acids within the P2X2 receptor C-terminus that regulate desensitization.
1999,
Pubmed
,
Xenbase Stoop,
Contribution of individual subunits to the multimeric P2X(2) receptor: estimates based on methanethiosulfonate block at T336C.
1999,
Pubmed
,
Xenbase Thomas,
The antagonist trinitrophenyl-ATP reveals co-existence of distinct P2X receptor channels in rat nodose neurones.
1998,
Pubmed Virginio,
Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors.
1998,
Pubmed Vulchanova,
Immunohistochemical study of the P2X2 and P2X3 receptor subunits in rat and monkey sensory neurons and their central terminals.
1997,
Pubmed Werner,
Domains of P2X receptors involved in desensitization.
1996,
Pubmed
,
Xenbase Xiang,
Localization of ATP-gated P2X receptor immunoreactivity in rat sensory and sympathetic ganglia.
1998,
Pubmed Zhong,
Pharmacological and molecular characterization of P2X receptors in rat pelvic ganglion neurons.
1998,
Pubmed
