Binding thermodynamics of serotonin to rat-brain 5-HT1A, 5HT2A and 5-HT3 receptors

The thermodynamic parameters delta G degrees, delta H degrees and delta S degrees 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 degrees C and van&...

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Bibliographic Details
Published inLife sciences (1973) Vol. 57; no. 12; pp. PL141 - A146
Main Authors Dalpiaz, A, Gessi, S, Borea, P A, Gilli, G
Format Journal Article
LanguageEnglish
Published Netherlands 11.08.1995
Subjects
Animals
Cerebral Cortex - physiology
In Vitro Techniques
Ligands
Protein Binding
Rats
Receptors, Serotonin - classification
Receptors, Serotonin - metabolism
Serotonin - metabolism
Thermodynamics
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Summary:The thermodynamic parameters delta G degrees, delta H degrees and delta S degrees 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 degrees 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.
ISSN:0024-3205
1879-0631
DOI:10.1016/0024-3205(95)02072-Q