Compounds > 3-aminopropylphosphinic-acid

3-aminopropylphosphinic-acid and Gastroesophageal-Reflux

3-aminopropylphosphinic-acid has been researched along with Gastroesophageal-Reflux* in 1 studies

Other Studies

1 other study(ies) available for 3-aminopropylphosphinic-acid and Gastroesophageal-Reflux

Article	Year
Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors. Journal of medicinal chemistry, 2008, Jul-24, Volume: 51, Issue:14 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 doses. We now report the discovery of atypical GABA B agonists devoid of classical GABA B agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug ( R)- 7 (AZD3355) that is presently being evaluated in man. Topics: Animals; Dose-Response Relationship, Drug; GABA Agonists; GABA-B Receptor Agonists; Gastroesophageal Reflux; Humans; Magnetic Resonance Spectroscopy; Spectrometry, Mass, Fast Atom Bombardment	2008

Article

Year

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

Journal of medicinal chemistry, 2008, Jul-24, Volume: 51, Issue:14

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 doses. We now report the discovery of atypical GABA B agonists devoid of classical GABA B agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug ( R)- 7 (AZD3355) that is presently being evaluated in man.

Topics: Animals; Dose-Response Relationship, Drug; GABA Agonists; GABA-B Receptor Agonists; Gastroesophageal Reflux; Humans; Magnetic Resonance Spectroscopy; Spectrometry, Mass, Fast Atom Bombardment

2008