Positron emission tomography study of [11C]methyl-tetrahydroaminoacridine (methyl-tacrine) in baboon brain
Autor: | Bertrand Tavitian, Antoinette Jobert, Christian Crouzel, Luigi Di Giamberardino, Sophie Bonnot-lours, C. Prenant, Sabina Pappatà |
---|---|
Rok vydání: | 1993 |
Předmět: |
Male
Cerebellum Biodistribution Pharmacology Rats Sprague-Dawley In vivo Cortex (anatomy) biology.animal Basal ganglia medicine Animals Tissue Distribution Binding Sites biology medicine.diagnostic_test business.industry Chemistry Brain Rats medicine.anatomical_structure Positron emission tomography Tacrine Injections Intravenous Acetylcholinesterase Cholinesterase Inhibitors Nuclear medicine business Papio Tomography Emission-Computed medicine.drug Baboon |
Zdroj: | European Journal of Pharmacology. 236:229-238 |
ISSN: | 0014-2999 |
DOI: | 10.1016/0014-2999(93)90593-7 |
Popis: | THA (1,2,3,4-tetrahydro-9-amino-acridine, tacrine), a potential therapeutic agent for patients suffering from Alzheimer's disease, has multiple pharmacological sites of action in the brain. In order to study the cerebral binding sites of THA in vivo, we labeled a close derivative of THA with carbon 11 for positron emission tomography (PET) analysis. We report the biodistribution of this compound, 1,2,3,4-tetrahydro-9-[11C]methylaminoacridine ([11C]MTHA), in the rodent and describe the first PET experiments in non-human primates. The distribution of [11C]MTHA in baboon brain, although rather diffuse in the gray matter, showed a higher concentration in the cortex and basal ganglia than in the cerebellum and binding could be displaced (50%) by cold THA. These results suggest that [11C]MTHA is a promising PET ligand for the study of the cerebral binding of THA. |
Databáze: | OpenAIRE |
Externí odkaz: |