[Pro34]peptide YY is a Y1-selective agonist at peptide YY/neuropeptide Y receptors

Eur J Pharmacol. 1994 Oct 14;269(2):127-32. doi: 10.1016/0922-4106(94)90078-7.

Abstract

We have investigated binding and functional effects of a new peptide YY analogue, [Pro34]peptide YY, at Y1 and Y2-like subtypes of receptors for peptide YY and neuropeptide Y. In binding studies [Pro34]peptide YY had a similarly high affinity as peptide YY to human Y1-like receptors in SK-N-MC cells, a human neuroblastoma cell line of presumed neurogenic origin, and HEL cells, a human cell line derived from a patient with Hodgkin's disease. In functional studies [Pro34]peptide YY stimulated Ca2+ elevations in both Y1-like receptor cell lines with similar potency and efficacy as peptide YY. In contrast to peptide YY [Pro34]peptide YY was 1000-fold less potent in binding to Y2-like receptors in porcine splenic membranes and lacked agonistic effects in another Y2-like receptor-mediated model system, i.e. inhibition of [3H]serotonin release from rat cerebral cortical slices. Thus, [Pro34]peptide YY is a highly Y1-selective full agonist of peptide YY/neuropeptide Y receptors. [Pro34]peptide YY could be useful for studying the importance of Y receptor subtypes in mediating peptide YY physiological actions.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding, Competitive / drug effects
  • Brain Neoplasms / metabolism
  • Calcium / metabolism
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Hodgkin Disease / metabolism
  • Humans
  • In Vitro Techniques
  • Molecular Sequence Data
  • Neuroblastoma / metabolism
  • Peptide YY*
  • Peptides / pharmacokinetics
  • Peptides / pharmacology*
  • Radioligand Assay
  • Rats
  • Receptors, Gastrointestinal Hormone / agonists*
  • Receptors, Gastrointestinal Hormone / biosynthesis
  • Receptors, Gastrointestinal Hormone / metabolism
  • Serotonin / metabolism
  • Swine
  • Tumor Cells, Cultured

Substances

  • Peptides
  • Receptors, Gastrointestinal Hormone
  • peptide YY receptor
  • peptide YY, Pro(34)-
  • Peptide YY
  • Serotonin
  • Calcium