Binding thermodynamics of serotonin to rat-brain 5-HT1a, 5HT2a and 5-HT3 receptors |
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| Affiliation: | 1. Dipartimento di Chimica Universita di Ferrara, 44100 Ferrara, Italy;2. Istituto di Farmacologia, Universita di Ferrara, 44100 Ferrara, Italy;1. Laboratory of Analytical Chemistry, Department of Chemistry, P.O. Box 55, FI-00014, University of Helsinki, Finland;2. Ridgeview Instruments AB, SE-740 20, Vänge, Sweden;3. Department of Immunology, Genetics and Pathology, Uppsala University, SE-75815, Uppsala, Sweden;4. Department of Engineering and Chemical Sciences, Karlstad University, SE-651 88, Karlstad, Sweden;5. Wihuri Research Institute, Haartmaninkatu 8, FI-00290, Helsinki, Finland;6. National Institute for Health and Welfare, Genomics and Biomarkers Unit, Biomedicum, FI-00290, Helsinki, Finland;1. Laboratory of Functional Biomolecules and Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Setsunan University, Osaka, Japan;2. Department of Cellular and Molecular Pharmacology, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima, Japan;1. Dept of Crystallography, University of Barcelona, Barcelona, Spain;2. Lab Food Technol Eng, Fac Biosci Eng, Ghent University, Gent, Belgium;3. Dept of Chem Biol, Ryerson University, Toronto, Ontario, Canada;4. Dept of Food Sci, Grad School Biosphere Sci., Hiroshima University, Higashi-Hiroshima, Japan;1. Protein Processing Section, Structural Biophysics Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA;2. Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, Minneapolis, MN 55455, USA;3. Biophysics Resource, Structural Biophysics Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA |
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| Abstract: | ![]()
The thermodynamic parameters ΔG° , ΔH° and Δs° of the binding equilibrium of serotonin to 5-HT1A, 5-HT2A and 5-HT3 rat-brain membrane receptors have been determined by means of affinity constant measurements at six temperatures in the range 0 –35 ° C and van't Hoff plots. At variance with 5-HT1A and 5-HT3, the binding at the 5-HT2A receptors is strongly endothermic and entropy-driven. Comparison with the results obtained by other authors on 5-HT2A receptors in rats and humans suggests that the observed differences can be explained by a single amino acid difference in the receptor sequence between these two species. |
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