Preparation and biological evaluation of 18F-labeled benzamide analogs as potential dopamine D2 receptor ligands
| Autor: | R Kawai, Meena Chelliah, Ronald G. Blasberg, Ernest S. Owens, Dale O. Kiesewetter, Catherine McLellan |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Fluorine Radioisotopes Erythrocytes Stereochemistry In Vitro Techniques Ligands Pyrrolidine Receptors Dopamine chemistry.chemical_compound Iodobenzamide Eticlopride In vivo Dopamine receptor D2 medicine Animals Humans Benzamide Fluoroethyl Raclopride Receptors Dopamine D2 Brain Rats Inbred Strains Blood Proteins General Medicine Rats chemistry Isotope Labeling Benzamides Protein Binding Tomography Emission-Computed medicine.drug |
| Zdroj: | International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology. 17:347-356 |
| ISSN: | 0883-2897 |
| Popis: | Three 18F-labeled benzamide derivatives were prepared and evaluated as potential ligands to study the dopamine D2 receptor phenomenon. The compounds are analogs of iodobenzamide, eticlopride and raclopride and are labeled with an N-2-[18F]fluoroethyl functionality on the pyrrolidine ring. The compounds were tested in vitro for binding affinity and found to exhibit somewhat lower affinity than the non-fluorinated analog. In vivo distribution studies revealed that all compounds were more highly bound to plasma proteins than was raclopride. In addition, compartmentation of radioactivity demonstrated nonspecific binding to be the predominate retention in the brain as reflected by the low caudate to cerebellum ratios for these compounds. These three 18F-labeled benzamide derivatives are inferior to raclopride and iodobenzamide for studies of the D2 receptor system using positron emission tomography. |
| Databáze: | OpenAIRE |
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