[(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 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.
Koscielniak
T
T
Service des Molécules marquées, C.E.A., C.E.N.-Saclay, Gif-sur-Yvette.
Ponchant
M
M
Laporte
A M
AM
Guminski
Y
Y
Verge
D
D
Hamon
M
M
Gozlan
H
H
D000818:Animals; D001345:Autoradiography; D001549:Benzamides / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D001665:Binding Sites; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002490:Central Nervous System / Q000737:chemistry*; D008024:Ligands; D051381:Rats; D011985:Receptors, Serotonin / Q000032:analysis*; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*
D001549:Benzamides; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D008024:Ligands; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C055971:zacopride
[125I]iodo-zacopride: un nouveau ligand pour l'étude par autoradiographie des récepteurs 5-HT3 centraux.