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.
Br J Pharmacol
2005 Jun 01;1453:313-22. doi: 10.1038/sj.bjp.0706187.
Show Gene links
Show Anatomy links
Antagonism of ATP responses at P2X receptor subtypes by the pH indicator dye, Phenol red.
King BF, Liu M, Townsend-Nicholson A, Pfister J, Padilla F, Ford AP, Gever JR, Oglesby IB, Schorge S, Burnstock G.
???displayArticle.abstract???
1 Many types of culture media contain a pH-sensitive dye. One commonly occurring dye, Phenol red sodium (Na(+)) salt, was tested for blocking activity at rat P2X(1-4) receptors (P2X(1-4)Rs) expressed in Xenopus oocytes. 2 Phenol red Na(+)-salt antagonised adenosine 5'-triphosphate (ATP) responses at P2X(1)R (IC(50), 3 microM) and, at higher concentrations, also blocked P2X(2)R and P2X(3)R. Phenol red Na(+)-salt, purified of lipophilic contaminants, blocked P2X(1)R and P2X(3)R by acting as an insurmountable antagonist. 3 Two lipophilic extracts of Phenol red antagonised ATP responses at P2XRs. Extract A was a potent antagonist at P2X(1)R (IC(50), 1.4 microM), whereas extract B was a potent antagonist at P2X(3)R (IC(50), 4.1 microM). A bisphenolic compound (RS151030) found in these extracts was a potent antagonist at P2X(1)R (IC(50), 0.3 microM) and at P2X(3)R (IC(50), 2.4 microM). 4 Phenolphthalein base was a potent irreversible antagonist at P2X(1)R (IC(50), 1 microM), whereas Phenolphthalein K(+)-salt was 25-fold less potent here. 5 Phenolphthalein base was a reversible antagonist of ATP responses at rat P2X(4)R (IC(50), 26 microM), whereas Phenolphthalein K(+)-salt was inactive. 6 Dimethyl sulphoxide (DMSO), used to dissolve lipophilic extracts, showed pharmacological activity by itself at rat P2X(1)R and P2X(4)R. 7 Thus, Phenol red and related compounds are antagonists at rat P2X(1)R, but are also active at other rat P2XRs. Phenolphthalein base is a newly identified, low potency antagonist of ATP responses at P2X(4)R. Culture media containing these red dyes should be used cautiously in future pharmacological studies of P2XRs. Also, wherever possible, the solvent DMSO should be used with caution.
Aschrafi,
Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypes.
2004, Pubmed,
Xenbase
Aschrafi,
Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypes.
2004,
Pubmed
,
Xenbase Berthois,
Phenol red in tissue culture media is a weak estrogen: implications concerning the study of estrogen-responsive cells in culture.
1986,
Pubmed Bindal,
Lipophilic impurities, not phenolsulfonphthalein, account for the estrogenic activity in commercial preparations of phenol red.
1988,
Pubmed Braun,
NF449: a subnanomolar potency antagonist at recombinant rat P2X1 receptors.
2001,
Pubmed
,
Xenbase Brown,
Activity of Novel Adenine Nucleotide Derivatives as Agonists and Antagonists at Recombinant Rat P2X Receptors.
2000,
Pubmed
,
Xenbase Brown,
Actions of a Series of PPADS Analogs at P2X1 and P2X3 Receptors.
2001,
Pubmed
,
Xenbase Buell,
An antagonist-insensitive P2X receptor expressed in epithelia and brain.
1996,
Pubmed Cass,
Phenolphthalein: a review of the medical literature and a controlled evaluation of its use as a laxative in the treatment of chronic constipation.
1965,
Pubmed Collo,
Cloning OF P2X5 and P2X6 receptors and the distribution and properties of an extended family of ATP-gated ion channels.
1996,
Pubmed Davies,
Ethanol sensitivity in ATP-gated P2X receptors is subunit dependent.
2002,
Pubmed
,
Xenbase Eaton,
Differential effects of dimethyl sulfoxide on nicotinic acetylcholine receptors from mouse muscle and Torpedo electrocytes.
1997,
Pubmed
,
Xenbase Ennion,
Agonist-stimulated internalisation of the ligand-gated ion channel P2X(1) in rat vas deferens.
2001,
Pubmed Ernst,
Phenol red mimics biological actions of estradiol: enhancement of osteoblast proliferation in vitro and of type I collagen gene expression in bone and uterus of rats in vivo.
1989,
Pubmed Grady,
pH-dependent cytotoxicity of contaminants of phenol red for MCF-7 breast cancer cells.
1991,
Pubmed Greenberg,
Phenol red is a thromboxane A2/prostaglandin H2 receptor antagonist in canine lingual arteries and human platelets.
1994,
Pubmed Honore,
TNP-ATP, a potent P2X3 receptor antagonist, blocks acetic acid-induced abdominal constriction in mice: comparison with reference analgesics.
2002,
Pubmed Hopp,
Lipophilic impurity of phenol red is a potent cation transport modulator.
1993,
Pubmed Jarvis,
A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat.
2002,
Pubmed Jiang,
Subunit arrangement in P2X receptors.
2003,
Pubmed Jones,
Functional regulation of P2X6 receptors by N-linked glycosylation: identification of a novel alpha beta-methylene ATP-sensitive phenotype.
2004,
Pubmed Khakh,
International union of pharmacology. XXIV. Current status of the nomenclature and properties of P2X receptors and their subunits.
2001,
Pubmed King,
Coexpression of rat P2X2 and P2X6 subunits in Xenopus oocytes.
2000,
Pubmed
,
Xenbase King,
A novel P1 purinoceptor activates an outward K+ current in follicular oocytes of Xenopus laevis.
1996,
Pubmed
,
Xenbase 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,
Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats.
2004,
Pubmed King,
P2 purinoceptor-activated inward currents in follicular oocytes of Xenopus laevis.
1996,
Pubmed
,
Xenbase Klapperstück,
Functional evidence of distinct ATP activation sites at the human P2X(7) receptor.
2001,
Pubmed
,
Xenbase Kym,
Bisphenolic compounds that enhance cell cation transport are found in commercial phenol red.
1996,
Pubmed Lambrecht,
The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors.
2000,
Pubmed
,
Xenbase Lewis,
2',3'-O-(2,4,6- trinitrophenyl) adenosine 5'-triphosphate (TNP-ATP)--a nanomolar affinity antagonist at rat mesenteric artery P2X receptor ion channels.
1998,
Pubmed Mullins,
Effects of internal sodium and hydrogen ions and of external calcium ions and membrane potential on calcium entry in squid axons.
1983,
Pubmed Nicke,
P2X1 and P2X3 receptors form stable trimers: a novel structural motif of ligand-gated ion channels.
1998,
Pubmed
,
Xenbase North,
Molecular physiology of P2X receptors.
2002,
Pubmed Nuttle,
Differential activation of cation channels and non-selective pores by macrophage P2z purinergic receptors expressed in Xenopus oocytes.
1994,
Pubmed
,
Xenbase Petrou,
P2X7 purinoceptor expression in Xenopus oocytes is not sufficient to produce a pore-forming P2Z-like phenotype.
1997,
Pubmed
,
Xenbase Raam,
Screening for hybridomas producing antibodies to steroid hormone receptors: interference from phenol red in the hybridoma culture supernates.
1992,
Pubmed Rettinger,
Roles of individual N-glycans for ATP potency and expression of the rat P2X1 receptor.
2000,
Pubmed
,
Xenbase Schorge,
Studies of NMDA receptor function and stoichiometry with truncated and tandem subunits.
2003,
Pubmed Valera,
A new class of ligand-gated ion channel defined by P2x receptor for extracellular ATP.
1994,
Pubmed
,
Xenbase Virginio,
Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors.
1998,
Pubmed Wildman,
Modulatory activity of extracellular H+ and Zn2+ on ATP-responses at rP2X1 and rP2X3 receptors.
1999,
Pubmed
,
Xenbase Wildman,
Sensitization by extracellular Ca(2+) of rat P2X(5) receptor and its pharmacological properties compared with rat P2X(1).
2002,
Pubmed
,
Xenbase Woodward,
Effects of the abused solvent toluene on recombinant P2X receptors expressed in HEK293 cells.
2004,
Pubmed Ziganshin,
Effects of P2-purinoceptor antagonists on degradation of adenine nucleotides by ecto-nucleotidases in folliculated oocytes of Xenopus laevis.
1996,
Pubmed
,
Xenbase Ziganshin,
Characteristics of ecto-ATPase of Xenopus oocytes and the inhibitory actions of suramin on ATP breakdown.
1995,
Pubmed
,
Xenbase
