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Molecular Pharmacology

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Research ArticleArticle

The Peptide YY-Preferring Receptor Mediating Inhibition of Small Intestinal Secretion Is a Peripheral Y2 Receptor: Pharmacological Evidence and Molecular Cloning

Mathieu Goumain, Thierry Voisin, Anne-Marie Lorinet, Robert Ducroc, Annick Tsocas, Claude Rozé, Patricia Rouet-Benzineb, Herbert Herzog, Ambikaipakan Balasubramaniam and Marc Laburthe
Molecular Pharmacology July 2001, 60 (1) 124-134; DOI: https://doi.org/10.1124/mol.60.1.124
Mathieu Goumain
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Thierry Voisin
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Anne-Marie Lorinet
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Robert Ducroc
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Annick Tsocas
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Claude Rozé
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Patricia Rouet-Benzineb
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Herbert Herzog
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Ambikaipakan Balasubramaniam
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Marc Laburthe
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Abstract

A peptide YY (PYY)-preferring receptor [PYY > neuropeptide Y (NPY)] was previously characterized in rat small intestinal crypt cells, where it mediates inhibition of fluid secretion. Here, we investigated the possible status of this receptor as a peripheral Y2 receptor in rats. Typical Y2 agonists (PYY3–36, NPY3–36, NPY13–36, C2-NPY) and very short PYY analogs (N-α-Ac-PYY22–36 andN-α-Ac-PYY25–36) acting at the intestinal PYY receptor were tested for their ability to inhibit the binding of125I-PYY to membranes of rat intestinal crypt cells and of CHO cells stably transfected with the rat hippocampal Y2 receptor cDNA. Similar PYY preference was observed and all analogs exhibited comparable high affinity in both binding assays. The same held true for the specific Y2 antagonist BIIE0246 with a K i value of 6.5 and 9.0 nM, respectively. BIIE0246 completely abolished the inhibition of cAMP production by PYY in crypt cells and transfected CHO cells. Moreover, the antagonist 1) considerably reversed the PYY-induced reduction of short-circuit current in rat jejunum mucosa in Ussing chamber and 2) completely abolished the antisecretory action of PYY on vasoactive intestinal peptide (VIP)-induced fluid secretion in rat jejunum in vivo. Quantitative reverse transcription-polymerase chain reaction (RT-PCR) experiments showed that Y2 receptor transcripts were present in intestinal crypt cells (3 × 102molecules/100 ng RNAT) with no expression in villus cells, in complete agreement with the exclusive binding of PYY in crypt cells. Finally, a full-length Y2 receptor was cloned by RT-PCR from rat intestinal crypt cells and also from human small intestine. We conclude that the so-called PYY-preferring receptor mediating inhibition of intestinal secretion is a peripheral Y2receptor.

  • Abbreviations

    PYY
    peptide YY
    NPY
    neuropeptide Y
    PP
    pancreatic polypeptide
    CHO
    Chinese hamster ovary
    p
    porcine
    r
    rat
    VIP
    vasoactive intestinal peptide
    KRB
    Krebs-Ringer buffer
    RT-PCR
    reverse transcription-polymerase chain reaction
    TBE
    Tris-borate EDTA
    bp
    base pair(s)
    TTX
    tetrodotoxin
    BIIE0246
    (S)-N2-[[1-[2-[4-[(R,S)-5,11-dihydro-6(6h)-oxodibenz[b,e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl] cyclopentyl] acetyl]-N-[2-[1,2-di-hydro-3,5-(4H)-dioxo-1,2-diphenyl-3H-1,2,4-triazol-4-yl]ethyl]-argininamid
    • Received November 28, 2000.
    • Accepted March 20, 2001.
    • The American Society for Pharmacology and Experimental Therapeutics
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    Molecular Pharmacology: 60 (1)
    Molecular Pharmacology
    Vol. 60, Issue 1
    1 Jul 2001
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    Research ArticleArticle

    The Peptide YY-Preferring Receptor Mediating Inhibition of Small Intestinal Secretion Is a Peripheral Y2 Receptor: Pharmacological Evidence and Molecular Cloning

    Mathieu Goumain, Thierry Voisin, Anne-Marie Lorinet, Robert Ducroc, Annick Tsocas, Claude Rozé, Patricia Rouet-Benzineb, Herbert Herzog, Ambikaipakan Balasubramaniam and Marc Laburthe
    Molecular Pharmacology July 1, 2001, 60 (1) 124-134; DOI: https://doi.org/10.1124/mol.60.1.124

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    Research ArticleArticle

    The Peptide YY-Preferring Receptor Mediating Inhibition of Small Intestinal Secretion Is a Peripheral Y2 Receptor: Pharmacological Evidence and Molecular Cloning

    Mathieu Goumain, Thierry Voisin, Anne-Marie Lorinet, Robert Ducroc, Annick Tsocas, Claude Rozé, Patricia Rouet-Benzineb, Herbert Herzog, Ambikaipakan Balasubramaniam and Marc Laburthe
    Molecular Pharmacology July 1, 2001, 60 (1) 124-134; DOI: https://doi.org/10.1124/mol.60.1.124
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