Synthesis and pharmacological evaluation of novel γ-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors

C Alstermark, K Amin, SR Dinn, T Elebring…

Index: Alstermark, Christer; Amin, Kosrat; Dinn, Sean R.; Elebring, Thomas; Fjellstroem, Ola; Fitzpatrick, Kevin; Geiss, William B.; Gottfries, Johan; Guzzo, Peter R.; Harding, James P.; Holmen, Anders; Kothare, Mohit; Lehmann, Anders; Mattsson, Jan P.; Nilsson, Karolina; Sunden, Gunnel; Swanson, Marianne; Von Unge, Sverker; Woo, Alex M.; Wyle, Michael J.; Zheng, Xiaozhang Journal of Medicinal Chemistry, 2008 , vol. 51, # 14 p. 4315 - 4320

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Citation Number: 35

Abstract

We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABAB agonists can produce CNS side ...