[125I]Leu31, Pro34-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: Evidence for heterogeneity in pancreatic polypeptide receptors

  • Gehlert D
  • Schober D
  • Gackenheimer S
 et al. 
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Abstract

Cloned receptors for the PP-fold peptides are subdivided into Y1, Y2, PP1/Y4, Y5 and Y6. NPY and PYY have similar affinity for Y1, Y2, Y5 and Y6 receptors while PP has highest affinity for PP1. Pro34-substituted analogs of NPY and PYY have selectivity for Y1 and Y1-like receptors over Y2 receptors. In the present study, we found the putative Y1-selective radioligand, [125I]Leu31, Pro34-PYY, also binds with high affinity to the rat PP1 receptor in cell lines expressing the receptor. However, in rat brain sections, [125I]Leu31, Pro34-PYY does not appear to bind to the interpeduncular nucleus, a brain region containing a high density of [125I]-bPP binding sites. Therefore, it appears there is additional heterogeneity in receptors recognizing PP.

Author-supplied keywords

  • Neuropeptide Y
  • Pancreatic polypeptide
  • Peptides
  • Radioligand
  • [125I]Leu31, Pro34-PYY

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Authors

  • Donald R. Gehlert

  • Douglas A. Schober

  • Susan L. Gackenheimer

  • Lisa Beavers

  • Robert Gadski

  • Ingrid Lundell

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