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Specific binding of 3N-(2′-[18F]fluoroethyl)benperidol to primate cerebral dopaminergic D2 receptors demonstrated in vivo by PET
| Content Provider | Semantic Scholar |
|---|---|
| Author | Moerlein, Stephen M. Perlmutter, Joel S. |
| Copyright Year | 1992 |
| Abstract | 3N-(2'-[18F]Fluoroethyl)benperidol ([18F]FEB) an 18F-labeled analogue of the D2 antagonist benperidol, was evaluated as a tracer for positron emission tomography (PET). PET imaging of a living baboon showed that the fluorinated ligand rapidly localized in vivo within D2 receptor-rich brain tissue, with selective retention lasting over 2 h after tracer injection. Pretreatment of the animal with unlabeled D2-specific antagonist eticlopride (4 mg/kg, i.v.) 1 h before [18F]FEB completely abolished the selective disposition of the radioligand, whereas the regional cerebral blood flow, blood volume and peripheral metabolism/protein binding of [18F]FEB were not changed. Tracer localization when the baboon was pretreated with unlabeled ketanserin (0.55 mg/kg, i.v.) or SCH 23390 (1.1 mg/kg, i.v.) was identical to that for the control case, indicating that the [18F]FEB did not bind to S2 of D1 receptors in vivo. [18F]FEB has advantages compared to previously used PET tracers, and may be an excellent radioligand for non-invasive study of D2 receptor binding. |
| Starting Page | 97 |
| Ending Page | 100 |
| Page Count | 4 |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/0304-3940(92)90813-M |
| PubMed reference number | 1300511 |
| Journal | Medline |
| Volume Number | 148 |
| Alternate Webpage(s) | https://api.elsevier.com/content/article/pii/030439409290813M |
| Alternate Webpage(s) | https://www.sciencedirect.com/science/article/pii/030439409290813M?dgcid=api_sd_search-api-endpoint |
| Alternate Webpage(s) | https://doi.org/10.1016/0304-3940%2892%2990813-M |
| Journal | Neuroscience Letters |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
