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A radioiodinated 7 α -O-iodoallyl diprenorphine for mapping opioid receptors |
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| Affiliation: | a Department of Nuclear Medicine, The First Hospital, Beijing Medical University, Beijing, P.R. of China;b Laboratoire d’imagerie Médicale Morphologique et Fonctionnelle (EA 826), Service de Biophysique et de Médecine Nucléaire, Faculité de Médecine Purpan, Toulouse;c Laboratoire de Pharmacologie et Toxicologie Fondamentales, CNRS 205, Toulouse, France |
| Abstract: | The aim of the current research has been to validate an original radioiodinated diprenorphine (DPN) derivative suitable for imaging studies of opioid receptors. [125I]7α-O-iodoallyl diprenorphine (7α-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 (Ki= 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 [125I]7α- 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). |
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