Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors

I Berque-Bestel, JL Soulier, M Giner…

Index: Berque-Bestel, Isabelle; Soulier, Jean-Louis; Giner, Mireille; Rivail, Lucie; Langlois, Michel; Sicsic, Sames Journal of Medicinal Chemistry, 2003 , vol. 46, # 13 p. 2606 - 2620

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Citation Number: 48

Abstract

Fluorescent antagonists for human 5-HT4 receptors were synthesized based on ML10302 1, a potent 5-HT4 receptor agonist and on piperazine analogue 2. These molecules were derived with three fluorescent moieties, dansyl, naphthalimide, and NBD (7-nitrobenz-2-oxa- 1, 3-diazol-4-yl), through alkyl chains. The synthesized molecules were evaluated in binding assays on the recently cloned human 5-HT4 (e) receptor isoform stably expressed in C6 ...