title: A radioiodinated 7alpha-O-iodoallyl diprenorphine for mapping opioid receptors.
abstract: The aim of the current research has been to validate an original radioiodinated diprenorphine (DPN) derivative suitable for imaging studies of opioid receptors. [(125)I]7alpha-O-iodoallyl diprenorphine (7alpha-O-IA-DPN) was prepared by radioiododestannylation and in vitro and in vivo opioid receptor binding assays were performed with CDF1 mouse brains. In vitro binding studies showed high affinity (K(i)= 0.4 +/- 0.2 nM) for mouse brain membranes. In vivo studies showed 63% specific binding. Ex vivo autoradiography of brain sections confirmed high uptake and retention of [(125)I]7alpha-O-IA-DPN in regions rich in opioid receptors. This new radioiodinated DPN analogue appears to be a potential radioprobe for in vivo visualization of human cerebral opioid receptors with single photon emission computed tomography (SPECT).
authors.affiliation: Department of Nuclear Medicine, The First Hospital, Beijing Medical University, Beijing, P.R. of China.
authors.forename: R F
authors.initials: RF
authors.lastname: Wang
authors.forename: J A
authors.initials: JA
authors.lastname: Tafani
authors.forename: J M
authors.initials: JM
authors.lastname: Zajac
authors.forename: R
authors.initials: R
authors.lastname: Guiraud
mesh_terms: D000818:Animals; D001345:Autoradiography; D001923:Brain Chemistry; D001931:Brain Mapping; D002540:Cerebral Cortex / Q000737:chemistry; D004174:Diprenorphine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007457:Iodine Radioisotopes; D008024:Ligands; D051379:Mice; D008815:Mice, Inbred Strains; D011869:Radioligand Assay / Q000379:methods*; D011957:Receptors, Opioid / Q000032:analysis* / Q000378:metabolism
chemical_list: C112739:I(123)-O-1A-diprenorphine; D007457:Iodine Radioisotopes; D008024:Ligands; D011957:Receptors, Opioid; D004174:Diprenorphine