Inhibition of serotonin transport by (+)McN5652 is noncompetitive
| Autor: | Pál Mikecz, Winfried Brenner, Malte Clausen, Oliver Schulze, Matthias Reimold, Thomas Rädler, Patrick Schloss, Ralph Buchert, René Hummerich |
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| Rok vydání: | 2006 |
| Předmět: |
Serotonin
Cancer Research medicine.medical_specialty Serotonin uptake Synaptic cleft Serotonin transport Kidney Serotonergic Binding Competitive chemistry.chemical_compound Internal medicine medicine Humans Radiology Nuclear Medicine and imaging Cells Cultured Serotonin transporter biology Isoquinolines Ligand (biochemistry) Protein Transport Endocrinology chemistry biology.protein Molecular Medicine Serotonin Antagonists McN5652 |
| Zdroj: | Nuclear Medicine and Biology. 33:317-323 |
| ISSN: | 0969-8051 |
| Popis: | Introduction Imaging of the serotonergic innervation of the brain using positron emission tomography (PET) with the serotonin transporter (SERT) ligand [ 11 C] (+)McN5652 might be affected by serotonin in the synaptic cleft if there is relevant interaction between [ 11 C] (+)McN5652 and serotonin at the SERT. The aim of the present study therefore was to pharmacologically characterize the interaction of [ 11 C] (+)McN5652 and serotonin at the SERT. Methods In vitro saturation analyses of [ 3 H]serotonin uptake into HEK293 cells stably expressing the human SERT were performed in the absence and presence of unlabelled (+)McN5652. Data were evaluated assuming Michaelis–Menten kinetics. Results Unlabelled (+)McN5652 significantly reduced the maximal rate of serotonin transport V max of SERT without affecting the Michaelis–Menten constant K M . Conclusions This finding indicates that (+)McN5652 inhibits serotonin transport through the SERT in a noncompetitive manner. This might suggest that [ 11 C] (+)McN5652 PET is not significantly affected by endogenous serotonin. |
| Databáze: | OpenAIRE |
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