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Simultaneous tritium labelling of two potent 5-HT4 ligands.

Abstract：

:Two potent and selective 5-HT(4) ligands, [(3)H]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyridine (1a) and [(3)H]-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-HT(4) ligands will allow for binding characterization as an essential tool for their further development.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Sobrio F,Lemaitre S,Hinsberger A,Barré L,Rousseau B,Rault S

doi

10.1016/j.ejmech.2009.12.012

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

1263-5

issue

3

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00638-2

journal_volume

45

pub_type

杂志文章

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