N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands

Nucl Med Biol. 2002 May;29(4):455-62. doi: 10.1016/s0969-8051(02)00300-1.

Abstract

The properties of two prospective positron emission tomography (PET) ligands for the delta-opioid receptor, N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) were investigated. Both were antagonists in the mouse vas deferens, and showed high affinity and selectivity, 1.81 nM and 3.09 nM respectively. [3H]BU97001 binding to rat whole brain was also of high affinity, K(D) of 0.42 nM of and B(MAX) of 59.95 fmol mg of protein(-1). In autoradiographic studies, it was found to bind to brain areas previously shown to be associated with the delta-opioid receptor and good correlations were found to exist with naltrindole and DPDPE. BU97018 and especially BU97001 appear to show good potential as delta-opioid receptor PET ligands with the incorporation of 18F.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoradiography
  • Binding Sites
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Dose-Response Relationship, Drug
  • Enkephalin, D-Penicillamine (2,5)- / metabolism*
  • In Vitro Techniques
  • Male
  • Mice
  • Naltrexone / analogs & derivatives*
  • Naltrexone / metabolism*
  • Naltrexone / pharmacology
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Receptors, Opioid, delta / metabolism*
  • Sensitivity and Specificity
  • Vas Deferens / diagnostic imaging
  • Vas Deferens / metabolism*

Substances

  • N1'-fluoroethyl-(14-formylamino)naltrindole
  • N1'-fluoroethyl-naltrindole
  • Radiopharmaceuticals
  • Receptors, Opioid, delta
  • Naltrexone
  • Enkephalin, D-Penicillamine (2,5)-
  • naltrindole