New arylpiperazine derivatives as antagonists of the human cloned 5-HT4 receptor isoforms

…, J Mialet, F Lezoualc'h, P Donzeau-Gouge…

Index: Curtet; Soulier; Zahradnik; Giner; Berque-Bestel; Mialet; Lezoualc'h; Donzeau-Gouge; Sicsic; Fischmeister; Langlois Journal of Medicinal Chemistry, 2000 , vol. 43, # 20 p. 3761 - 3769

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Citation Number: 12

Abstract

New derivatives of arylpiperazine 9 were designed from ML 10302, a potent 5-HT4 receptor agonist in the gastrointestinal system. Compounds were synthesized by condensation of a number of available arylpiperazines or heteroarylpiperazines with 2-bromoethyl 4-amino-5- chloro-2-methoxybenzoate. They were evaluated in binding assays on the recently cloned human 5-HT4 (e) isoform stably expressed in C6 glial cells with [3H] GR 113808 as the ...