(125I)iodo-zacopride: new ligand for the study by autoradiography of central 5-HT3 receptors |
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| Authors: | T Koscielniak M Ponchant A M Laporte Y Guminski D Verge M Hamon H Gozlan |
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| Institution: | Service des Molécules marquées, C.E.A., C.E.N.-Saclay, Gif-sur-Yvette. |
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| Abstract: | 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. |
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