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PMID:8891585

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Citation

Dalpiaz, A, Borea, PA, Gessi, S and Gilli, G (1996) Binding thermodynamics of 5-HT1A receptor ligands. Eur. J. Pharmacol. 312:107-14

Abstract

The thermodynamic parameters delta G degree, delta H degree and delta S degree of the binding equilibrium of 15 ligands (eight agonists and seven antagonists) to the 5-HT1A receptor subtype have been determined by affinity measurements carried out on rat cortex membranes (minus striatum) at six different temperatures (0, 10, 20, 25, 30, 35 degrees C), and by van't Hoff plots. Most of the compounds studied are tryptamine, phenylpiperazine and tetralin derivatives. Affinity constants were measured by saturation experiments for the selective 5-HT1A receptor agonist [3H]8-hydroxy-N,N-dipropyl-2-aminotetralin ([3H]8-OH-DPAT) and by inhibition assays of [3H]8-OH-DPAT binding for the other compounds. Scatchard plots were monophasic in the full range of temperatures, indicating a single class of high affinity binding sites. Van't Hoff plots of all ligands were linear in the temperature range investigated (0-30 degrees C or 0-35 degrees C). 5-Hydroxytryptamine (serotonin) and 5-methoxy-tryptamine (mexamine) displayed a positive slope. Experimental data indicate that for 5-HT1A receptor subtype agonists and antagonists are not thermodynamically discriminated. The results are discussed from a quantitative point of view with the aim of obtaining new details on the nature of the forces driving the 5-HT1A binding at a molecular level.

Links

PubMed

Keywords

8-Hydroxy-2-(di-n-propylamino)tetralin/metabolism; Animals; Cerebral Cortex/metabolism; Ligands; Male; Rats; Rats, Wistar; Receptors, Serotonin/metabolism; Serotonin Antagonists/metabolism; Serotonin Receptor Agonists/metabolism; Temperature; Thermodynamics

Significance

Annotations

Gene product Qualifier GO Term Evidence Code with/from Aspect Extension Notes Status

RAT:5HT1A

enables

GO:0008144: drug binding

ECO:0000314: direct assay evidence used in manual assertion

F

Seeded From UniProt

complete

RAT:5HT1A

part_of

GO:0016020: membrane

ECO:0000314: direct assay evidence used in manual assertion

C

Seeded From UniProt

complete

RAT:5HT1A

enables

GO:0051378: serotonin binding

ECO:0000314: direct assay evidence used in manual assertion

F

Seeded From UniProt

complete

Notes

See also

References

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