Discovery and pharmacological profile of new hydrophilic 5-HT4 receptor antagonists

作者：Brudeli Bjarne; Navaratnarajah Mirusha; Andressen Kjetil Wessel; Manfra Ornella; Moltzau Lise Roman; Nilsen Nils Olav; Levy Finn Olav; Klaveness Jo^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(18): 4598-4602.

DOI：10.1016/j.bmcl.2014.06.083

• 5-HT4 receptor antagonists
• hERG
• Pharmacokinetic

The synthesis and pharmacological data of some new and potent hydrophilic 5-HT4 receptor antagonists are described. Propanediol derivative 25 was identified as a potent antagonist with low affinity for the hERG potassium channel and promising pharmacokinetics.

• 出版日期2014-9-15