Design and evaluation of radioactive acetylcholine analogs for mapping brain acetylcholinesterase (AchE) in vivo
| Autor: | Toshiaki Irie, Hiroshi Tamagami, Tadashi Nozaki, Kiyoshi Fukushi, Yoshio Akimoto |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Male
Cancer Research Magnetic Resonance Spectroscopy Aché Metabolite Butyrate Substrate Specificity chemistry.chemical_compound Mice In vivo medicine Animals Radiology Nuclear Medicine and imaging Carbon Radioisotopes Propionates chemistry.chemical_classification Mice Inbred C3H Brain Acetylcholinesterase language.human_language Acetylcholine Enzyme Biochemistry chemistry Regional Blood Flow language Molecular Medicine medicine.drug |
| Zdroj: | Nuclear medicine and biology. 21(6) |
| ISSN: | 0969-8051 |
| Popis: | For mapping brain acetylcholinesterase (AchE) in vivo , seven radioactive acetylcholine analogs, N -[ 14 C]methylpiperidyl-3-and 4-acetates, propionates, isobutyrates, and 3-butyrate were newly synthesized and evaluated in mice. The esters readily entered the brain and were hydrolyzed into the hydrophilic metabolite, which was trapped. In brain homogenates, the esters showed a wide range of enzymatic reactivity (about 40-fold), and high specificity for AchE (more than 82%) except the butyrate. Intra-brain distribution of the esters reflected a pattern of AchE activity. |
| Databáze: | OpenAIRE |
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