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

@article{Alstermark2008SynthesisAP,
  title={Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors.},
  author={Christer Alstermark and Kosrat Amin and Sean R. Dinn and Thomas Elebring and Ola Fjellstr{\"o}m and Kevin Fitzpatrick and William B Geiss and Johan Gottfries and Peter R. Guzzo and J. Patrick Harding and Anders G Holm{\'e}n and Mohit A Kothare and Anders Lehmann and Jan P. Mattsson and Karolina Nilsson and Gunnel Sund{\'e}n and Marianne Swanson and Sverker von Unge and Alex M Woo and M. Jentoft-Nilsen Wyle and Xiaozhang Zheng},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 14},
  pages={4315-20}
}
We have previously demonstrated that the prototypical GABA B receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABA B agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABA B agonists can produce CNS side effects such as sedation, dizziness, nausea, and vomiting at higher… CONTINUE READING

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