☆ 4.7 Article

Simultaneous tritium labelling of two potent 5-HT4 ligands

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

卷 45, 期 3, 页码 1263-1265

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

DOI: 10.1016/j.ejmech.2009.12.012

关键词

Tritium; Radiolabelling; Radioligand; 5-HT4; Serotonin-4 receptors

类别

Chemistry, Medicinal

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摘要

Two potent and selective 5-HT4 ligands, [H-3]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyricline (1a) and [H-3]-1-methyl-5-[(N-propylpiperidin-4-yl)methoxy]pyrrolo[1,2-a]thieno[2,3-e]pyrazine (2a) were radiolabelled with tritium. Radioactive labelling was achieved by Simultaneous tritium reduction of a mixture of both propargylic precursors (1c-2c). The two tritiated ligands thus obtained were radiochemically pure and possessed high radioactive specific activities. These tritiated 5-HT4 ligands will allow for binding characterization as an essential tool for their further development. (C) 2009 Elsevier Masson SAS. All rights reserved.

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