N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands.
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.
Tyacke
Robin J
RJ
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, UK.
Robinson
Emma S J
ES
Schnabel
Rebecca
R
Lewis
John W
JW
Husbands
Stephen M
SM
Nutt
David J
DJ
Hudson
Alan L
AL
D000818:Animals; D001345:Autoradiography; D001665:Binding Sites; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D017465:Receptors, Opioid, delta / Q000378:metabolism*; D012680:Sensitivity and Specificity; D014649:Vas Deferens / Q000000981:diagnostic imaging / Q000378:metabolism*
C469346:N1'-fluoroethyl-(14-formylamino)naltrindole; C469345:N1'-fluoroethyl-naltrindole; D019275:Radiopharmaceuticals; D017465:Receptors, Opioid, delta; D009271:Naltrexone; D020881:Enkephalin, D-Penicillamine (2,5)-; C055382:naltrindole