Synthesis and Structure–Affinity Relationships of Selective High-Affinity 5-HT4 Receptor Antagonists: Application to the Design of New Potential Single Photon …

…, F Dulin, J Sopkova de-Oliveira Santos…

文献索引：Dubost, Emmanuelle; Dumas, Noe; Fossey, Christine; Magnelli, Rosa; Butt-Gueulle, Sabrina; Ballandonne, Celine; Caignard, Daniel H.; Dulin, Fabienne; Sopkova De-Oliveira Santos, Jana; Millet, Philippe; Charnay, Yves; Rault, Sylvain; Cailly, Thomas; Fabis, Frederic Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9693 - 9707

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被引用次数: 29

摘要

The work described herein aims at finding new potential ligands for the brain imaging of 5- HT4 receptors (5-HT4Rs) using single-photon emission computed tomography (SPECT). Starting from the nonsubstituted phenanthridine compound 4a, exhibiting a K i value of 51 nM on the 5-HT4R, we explored the structure–affinity in this series. We found that substitution in position 4 of the tricycle with a fluorine atom gave the best result. ...