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[3H]-GR113808 labels 5-HT4 receptors in the human and guinea-pig brain
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[3H]-GR113808 labels 5-HT4 receptors in the human and guinea-pig brain

Christian Waeber, Michèle Sebben, Carol Grossman, France Javoy-Agid, Joël Bockaert et Aline Dumuis
Neuroreport, Vol.4(11), p.1239-1242
10/09/1993
PMID: 8219020

Résumé

A TRITIATED specific and highly potent 5-HT4 antagonist[H]-GR113808 was used to label specific binding sites in human brain and for comparison in guinea-pig brain. [H]-GR113808 association and dissociation were rapid, the binding was saturable and displaced by various sero-toninergic agents with an affinity corresponding to their previously reported 5-HT receptor mediated effects. In vitro ligand binding autoradiography was used to investigate the distribution of [H]-GR113808 recognition sites on human brain sections. The highest density was observed in the striato-nigral system. Low densities of binding sites were also found in hippocampus, neocortex and colliculus. This distribution of [H]-GR113808 binding sites is similar to that found in the guinea-pig brain.

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