Literature DB >> 17928736

The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities.

Tetsuo Toga1, Yumi Kohmura, Ryoichi Kawatsu.   

Abstract

The blocking effect of three 5-HT(4) agonists, cisapride, mosapride, and the newly discovered CJ-033466 on the human ether-a-go-go-related gene (hERG) channel was studied using a whole cell patch-clamp technique in HEK293 cells. Cisapride was found to be the most potent of the hERG blockers. CJ-033466 had the widest safety margin between its hERG blocking activity and 5-HT(4) agonism among the tested compounds. This suggests a lower clinical risk of cardiac arrhythmia in CJ-033466 compared with the other 2 agonists. Therefore, CJ-033466 has the potential to be a drug with higher therapeutic efficacy and less cardiac risk than both cisapride and mosapride.

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Year:  2007        PMID： 17928736     DOI： 10.1254/jphs.sc0070243

Source DB:  PubMed          Journal:  J Pharmacol Sci        ISSN： 1347-8613            Impact factor:   3.337


  10 in total

Review 1.  Efficacy of mosapride plus proton pump inhibitors for treatment of gastroesophageal reflux disease: a systematic review.

Authors:  Qing Liu; Chen-Chen Feng; Er-Man Wang; Xiu-Juan Yan; Sheng-Liang Chen
Journal:  World J Gastroenterol       Date:  2013-12-21       Impact factor: 5.742

2.  Effects of mosapride on esophageal motor activity and esophagogastric junction compliance in healthy volunteers.

Authors:  Kousuke Fukazawa; Kenji Furuta; Kyoichi Adachi; Yoshiya Moritou; Tsukasa Saito; Ryusaku Kusunoki; Goichi Uno; Shino Shimura; Masahito Aimi; Shunji Ohara; Shunji Ishihara; Yoshikazu Kinoshita
Journal:  J Gastroenterol       Date:  2013-09-07       Impact factor: 7.527

Review 3.  Mosapride in gastrointestinal disorders.

Authors:  Monique P Curran; Dean M Robinson
Journal:  Drugs       Date:  2008       Impact factor: 9.546

4.  Iatrogenic QT Abnormalities and Fatal Arrhythmias: Mechanisms and Clinical Significance.

Authors:  Luigi X Cubeddu
Journal:  Curr Cardiol Rev       Date:  2009-08

5.  High throughput measurement of Ca²⁺ dynamics for drug risk assessment in human stem cell-derived cardiomyocytes by kinetic image cytometry.

Authors:  Fabio Cerignoli; David Charlot; Ross Whittaker; Randy Ingermanson; Piyush Gehalot; Alex Savchenko; David J Gallacher; Rob Towart; Jeffrey H Price; Patrick M McDonough; Mark Mercola
Journal:  J Pharmacol Toxicol Methods       Date:  2012-08-25       Impact factor: 1.950

6.  Neuronal stimulation with 5-hydroxytryptamine 4 receptor induces anti-inflammatory actions via α7nACh receptors on muscularis macrophages associated with postoperative ileus.

Authors:  Yasuaki Tsuchida; Fumihiko Hatao; Masahiko Fujisawa; Takahisa Murata; Michio Kaminishi; Yasuyuki Seto; Masatoshi Hori; Hiroshi Ozaki
Journal:  Gut       Date:  2010-11-29       Impact factor: 23.059

Review 7.  Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders.

Authors:  J Tack; M Camilleri; L Chang; W D Chey; J J Galligan; B E Lacy; S Müller-Lissner; E M M Quigley; J Schuurkes; J H De Maeyer; V Stanghellini
Journal:  Aliment Pharmacol Ther       Date:  2012-02-22       Impact factor: 8.171

8.  Rehabilitating drug-induced long-QT promoters: in-silico design of hERG-neutral cisapride analogues with retained pharmacological activity.

Authors:  Serdar Durdagi; Trevor Randall; Henry J Duff; Adam Chamberlin; Sergei Y Noskov
Journal:  BMC Pharmacol Toxicol       Date:  2014-03-08       Impact factor: 2.483

Review 9.  New Aspects of Bilayer Lipid Membranes for the Analysis of Ion Channel Functions.

Authors:  Hironori Kageyama; Teng Ma; Madoka Sato; Maki Komiya; Daisuke Tadaki; Ayumi Hirano-Iwata
Journal:  Membranes (Basel)       Date:  2022-09-06

10.  A structure-based computational workflow to predict liability and binding modes of small molecules to hERG.

Authors:  Subha Kalyaanamoorthy; Shawn M Lamothe; Xiaoqing Hou; Tae Chul Moon; Harley T Kurata; Michael Houghton; Khaled H Barakat
Journal:  Sci Rep       Date:  2020-10-01       Impact factor: 4.379
  10 in total

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