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OtherCELLULAR AND MOLECULAR PHARMACOLOGY

Antagonism of an Adenosine/ATP Receptor in FollicularXenopus Oocytes

B. F. King, S. S. Wildman, A. Townsend-Nicholson and G. Burnstock
Journal of Pharmacology and Experimental Therapeutics June 1998, 285 (3) 1005-1011;
B. F. King
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S. S. Wildman
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A. Townsend-Nicholson
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G. Burnstock
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Abstract

Follicular Xenopus oocytes possess a novel receptor where both adenosine and ATP activate a cAMP-dependent, nonrectifying K+-current. Five compounds, α,β-methylene ATP (α,β-meATP), 8-(p-sulfophenyl)theophylline (8-SPT), theophylline, 2,2′-pyridylisatogen tosylate (PIT) and suramin, were tested as antagonists of adenosine- and ATP-activated K+-currents. The descending order of activity (pIC50 values) against adenosine responses was: α,β-meATP (6.72) = 8-SPT (6.68) > theophylline (5.32) > PIT (4.58), whereas suramin was relatively inactive. The blocking actions of α,β-meATP and alkylxanthine compounds were reversible with washout, whereas blockade by PIT was irreversible. These antagonists showed similar blocking activity against ATP responses, except for PIT which was more effective at ATP responses than at adenosine responses. The selectivity of antagonists was tested against cAMP-dependent K+-currents evoked by forskolin and follicle-stimulating hormone (FSH). 8-SPT and theophylline did not inhibit but instead augmented forskolin and FSH responses; this augmentation may be caused by inhibition of phosphodiesterase activity inside follicle cells. On the other hand, α,β-MeATP and PIT inhibited forskolin and FSH responses; both compounds apparently are nonselective antagonists. Thus, only alkylxanthine derivatives (8-SPT and theophylline) were selective antagonists of the novel adenosine/ATP receptor inXenopus oocytes, whereas α,β-meATP and PIT were nonselective in their blocking actions and suramin was relatively inactive.

Footnotes

  • Send reprint requests to: Brian F. King, PhD, Department of Anatomy and Developmental Biology, University College London, Gower Street, London WC1E 6BT, England.

  • ↵1 This work was supported by the British Heart Foundation and Institut de Recherches Internationales Servier (France).

  • ↵2 The authors are also affiliated with: Autonomic Neuroscience Institute, Royal Free Hospital School of Medicine, Rowland Hill Street, Hampstead, London NW3 2PF, England.

  • Abbreviations:
    AC
    adenylate cyclase
    ATP
    adenosine 5′-triphosphate
    α
    β-meATP, α,β-methyleneATP
    β
    γ-meATP, β,γ-methyleneATP
    cAMP
    adenosine 3′5′-cyclic monophosphate
    Erev
    reversal potential
    FSH
    follicle-stimulating hormone
    NECA
    5′-N-ethylcarboxamide-adenosine
    PDE
    phosphodiesterase
    pIC50
    −logIC50 value
    PIT
    2,2′-pyridylisatogen tosylate
    8-SPT
    8-(p-sulfophenyl)theophylline
    TEA
    tetraethylammonium ions
    Vh
    holding potential
    HEPES
    N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid
    • Received July 28, 1997.
    • Accepted February 9, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics
Vol. 285, Issue 3
1 Jun 1998
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OtherCELLULAR AND MOLECULAR PHARMACOLOGY

Antagonism of an Adenosine/ATP Receptor in FollicularXenopus Oocytes

B. F. King, S. S. Wildman, A. Townsend-Nicholson and G. Burnstock
Journal of Pharmacology and Experimental Therapeutics June 1, 1998, 285 (3) 1005-1011;

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OtherCELLULAR AND MOLECULAR PHARMACOLOGY

Antagonism of an Adenosine/ATP Receptor in FollicularXenopus Oocytes

B. F. King, S. S. Wildman, A. Townsend-Nicholson and G. Burnstock
Journal of Pharmacology and Experimental Therapeutics June 1, 1998, 285 (3) 1005-1011;
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  • Inhibition of Voltage-Dependent Sodium Channels by the Anticonvulsant γ-Aminobutyric Acid Type A Receptor Modulator, 3-Benzyl-3-Ethyl-2-Piperidinone
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