High-yielding 18F radiosynthesis of a novel oxytocin receptor tracer, a probe for nose-to-brain oxytocin uptake in vivo

Chem Commun (Camb). 2018 Jul 17;54(58):8120-8123. doi: 10.1039/c8cc01400k.

Abstract

A novel Al18F labelled peptide tracer for PET imaging of oxytocin receptor has been accessed through a high radiochemical yield approach. This tracer showed comparable affinity and higher selectivity and stability compared to oxytocin, and was used to demonstrate direct nose-to-brain uptake following intranasal administration, a common yet controversial delivery route for oxytocin-based therapeutics.

MeSH terms

  • Administration, Intranasal
  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Female
  • Fluorine Radioisotopes
  • Half-Life
  • Heterocyclic Compounds, 1-Ring / administration & dosage
  • Heterocyclic Compounds, 1-Ring / chemical synthesis
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Heterocyclic Compounds, 1-Ring / pharmacokinetics*
  • Male
  • Olfactory Bulb / diagnostic imaging
  • Olfactory Bulb / metabolism
  • Peptides, Cyclic / administration & dosage
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacokinetics*
  • Positron-Emission Tomography
  • Radiopharmaceuticals / administration & dosage
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats, Wistar
  • Receptors, Oxytocin / metabolism*
  • Structure-Activity Relationship

Substances

  • Fluorine Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Peptides, Cyclic
  • Radiopharmaceuticals
  • Receptors, Oxytocin