Fluorescent agonists and antagonists for vasopressin/oxytocin G protein-coupled receptors: usefulness in ligand screening assays and receptor studies

Mini Rev Med Chem. 2008 Sep;8(10):996-1005. doi: 10.2174/138955708785740607.

Abstract

Different series of fluorescent agonists and antagonists have been developed and characterized for arginine-vasopressin and oxytocin G protein-coupled receptors. Both cyclic and linear peptide analogs of the neurohypophysial hormones are useful tools for investigating receptor localization and trafficking, analysing receptor structural organization, and developing new receptor-selective high-throughput ligand screening assays.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists
  • Antigens, Differentiation / metabolism
  • Drug Evaluation, Preclinical / methods
  • Fluorescent Dyes / pharmacology*
  • Receptors, G-Protein-Coupled / agonists*
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Oxytocin / agonists
  • Receptors, Oxytocin / antagonists & inhibitors
  • Receptors, Oxytocin / metabolism
  • Receptors, Vasopressin / agonists
  • Receptors, Vasopressin / metabolism

Substances

  • Antidiuretic Hormone Receptor Antagonists
  • Antigens, Differentiation
  • Fluorescent Dyes
  • Receptors, G-Protein-Coupled
  • Receptors, Oxytocin
  • Receptors, Vasopressin