Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties

Bioorg Med Chem Lett. 2004 Jan 19;14(2):369-72. doi: 10.1016/j.bmcl.2003.11.001.

Abstract

[(3)H]BBL454, a new CCK(2) selective tritiated agonist was prepared via the reductive tritiation of a 5-aminopentyn-1-yl moiety introduced on the N-terminal end of a pentapeptide derivative of cholecystokinin. The binding properties of this labelled compound were determined on CHO cells transfected with the rat CCK(2) receptor. [(3)H]BBL454 is able to discriminate two affinity states of the CCK(2) receptor a supplementary indication of its validity for further exploring the heterogeneity of this receptor.

MeSH terms

  • Animals
  • CHO Cells
  • Cholecystokinin / analogs & derivatives
  • Cholecystokinin / chemical synthesis*
  • Cholecystokinin / metabolism*
  • Cricetinae
  • Guinea Pigs
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / metabolism
  • Peptide Fragments / chemical synthesis*
  • Peptide Fragments / metabolism*
  • Radioligand Assay / methods
  • Rats
  • Receptor, Cholecystokinin B / agonists*
  • Receptor, Cholecystokinin B / metabolism
  • Tritium / metabolism

Substances

  • (3H)BBL454, peptide
  • Oligopeptides
  • Peptide Fragments
  • Receptor, Cholecystokinin B
  • Tritium
  • Cholecystokinin