(125I)iodo-zacopride: new ligand for the study by autoradiography of central 5-HT3 receptors

(125I)iodo-zacopride: new ligand for the study by autoradiography of central 5-HT3 receptors

This paper describes the synthesis and the pharmacological characteristics of the first radioiodinated ligand of central 5-HT3 receptors: [125I]iodo-zacopride. Specific sites having a high affinity (Kd = 4.3 nM) for [125I]iodo-zacopride have been found in membranes from the rat entorhinal cortex. In...

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Veröffentlicht in:Comptes rendus de l'Académie des sciences, Série III, Sciences de la vie Série III, Sciences de la vie, 1990, Vol.311 (6), p.231-237
Hauptverfasser: Koscielniak, T, Ponchant, M, Laporte, A M, Guminski, Y, Verge, D, Hamon, M, Gozlan, H
Format: Artikel
Sprache:fre
Schlagworte:
Animals
Autoradiography
Benzamides - chemical synthesis
Benzamides - pharmacokinetics
Benzamides - pharmacology
Binding Sites
Bridged Bicyclo Compounds - chemical synthesis
Bridged Bicyclo Compounds - pharmacokinetics
Bridged Bicyclo Compounds - pharmacology
Bridged Bicyclo Compounds, Heterocyclic
Central Nervous System - chemistry
Ligands
Rats
Receptors, Serotonin - analysis
Serotonin Antagonists - chemical synthesis
Serotonin Antagonists - pharmacokinetics
Serotonin Antagonists - pharmacology
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Zusammenfassung:This paper describes the synthesis and the pharmacological characteristics of the first radioiodinated ligand of central 5-HT3 receptors: [125I]iodo-zacopride. Specific sites having a high affinity (Kd = 4.3 nM) for [125I]iodo-zacopride have been found in membranes from the rat entorhinal cortex. In addition, a highly significant correlation (r = 0.995) existed between the Ki of several 5-HT-related drugs for displacing both [125I]iodo-zacopride from its specific binding sites, and [3H]zacopride from 5-HT3 receptors. Finally, [125I]iodo-zacopride was successfully used for the autoradiographic mapping of 5-HT3 receptors in the rat central nervous system.
ISSN:0764-4469