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

Peptides. 1997;18(3):397-401. doi: 10.1016/s0196-9781(96)00346-4.

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.

MeSH terms

  • Animals
  • Brain / metabolism
  • CHO Cells
  • Cricetinae
  • Gastrointestinal Hormones / metabolism*
  • Iodine Radioisotopes
  • Ligands
  • Neuropeptide Y / analogs & derivatives*
  • Neuropeptide Y / chemistry
  • Neuropeptide Y / metabolism
  • Neuropeptide Y / physiology
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism
  • Rats
  • Receptors, Neuropeptide Y / chemistry
  • Receptors, Neuropeptide Y / metabolism*
  • Receptors, Pancreatic Hormone / chemistry
  • Receptors, Pancreatic Hormone / metabolism*
  • Recombinant Proteins

Substances

  • Gastrointestinal Hormones
  • Iodine Radioisotopes
  • Ligands
  • Neuropeptide Y
  • Peptide Fragments
  • Receptors, Neuropeptide Y
  • Receptors, Pancreatic Hormone
  • Recombinant Proteins
  • neuropeptide Y-Y1 receptor
  • peptide YY, iodo-Leu(34)-Pro(34)-
  • neuropeptide Y, Leu(31)-Pro(34)-