Synthesis and in vitro binding properties of halogenated analogues of GBR as new dopamine uptake carrier ligands
| Autor: | Y. Frangin, G. Desplanches, Sylvie Chalon, Jean-Claude Besnard, Jean-Louis Baulieu, Denis Guilloteau, C. Foulon, Lucette Garreau |
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| Rok vydání: | 1992 |
| Předmět: |
animal structures
Stereochemistry Dopamine Ligands High-performance liquid chromatography Piperazines Iodine Radioisotopes chemistry.chemical_compound In vivo medicine Animals heterocyclic compounds Radionuclide Imaging Binding Sites Chemistry virus diseases Brain General Medicine GBR-12935 In vitro In vitro binding Rats Piperazine Membrane Isotope Labeling Bromine Radioisotopes medicine.drug |
| Zdroj: | International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology. 19(5) |
| ISSN: | 0883-2897 |
| Popis: | We present the original synthesis of two halogenated analogues of the diphenyl piperazine GBR, bromo-GBR and iodo-GBR, as new dopamine uptake carrier ligands. The derivatives were purified by HPLC and chemically characterized. Bromo-GBR and iodo-GBR and iodo-GBR are potent inhibitors of [3H]GBR 12935 binding to rat striatal membrane, with Ki values of 116 and 113 nM, respectively. We prepared iodo-GBR labeled with iodide-125 from the brominated derivative and concluded that [123I]iodo-GBR could be a potential tool to explore the in vivo dopamine uptake carrier. |
| Databáze: | OpenAIRE |
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