Receptor mapping using methoxy phenyl piperazine derivative: Preclinical PET imaging
| Autor: | Meganathan Thirumal, Anupama Datta, Anjani K. Tiwari, K. Ganesh Kadiyala, Garima Mann |
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| Rok vydání: | 2021 |
| Předmět: |
Biodistribution
Pharmacology Ligands Receptors Metabotropic Glutamate Biochemistry Piperazines chemistry.chemical_compound Mice Drug Discovery Animals Humans Tissue Distribution Receptor Molecular Biology Mice Inbred BALB C Molecular Structure Organic Chemistry Brain Ligand (biochemistry) Haemolysis Healthy Volunteers Rats Piperazine chemistry Metabotropic glutamate receptor Positron-Emission Tomography Metabotropic glutamate receptor 1 Specific activity |
| Zdroj: | Bioorganic chemistry. 117 |
| ISSN: | 1090-2120 |
| Popis: | This study aimed at assessing 2-methoxyphenyl piperazine derivative for its binding specificity and suitability in mapping metabotropic glutamate receptor subtype 1, which is implicated in several neuropsychiatric disorders. N-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-N-methylpyridin-2-amine was synthesised and evaluated for brain imaging subsequent to radiolabelling with [11C] radioisotope via methylation process in 98.9% purity and 52 ± 6% yield (decay corrected). The specific activity was in the range of 72–93 GBq/µmol. The haemolysis of blood was 2–5% for initial 4 hr and remained The PET as well as biodistribution studies also showed high activity in the brain with a direct correlation between receptor abundance distribution pattern and tracer activity. The biodistribution analyses revealed initial high brain uptake (4.18 ± 0.48). The highest uptake was found in cerebellum (SUV 4.7 ± 0.2), followed by thalamus (SUV 3.5 ± 0.1), and striatum (SUV 3 ± 0.1). In contrast, pons had negligible tracer activity. The high uptake observed in all the regions with known mGluR1 activity indicates suitability of the ligand for mGluR1 imaging. |
| Databáze: | OpenAIRE |
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