Novel GABA(B) receptor positive modulators: a patent survey

Expert Opinion on Therapeutic Patents
W Froestl

Abstract

Positive allosteric modulators of GABA(B) receptors may have a similar potential as positive modulators of GABA(A) receptors, the benzodiazepines discovered in 1957. The discovery of positive allosteric modulators of GABA(B) receptors at Novartis in Basel in 2000 opened the way to search for compounds, which activate GABA(B) receptors without the drawbacks of full agonists, such as desensitization, tolerance, muscle-relaxant effects, hypothermia, and central and gastrointestinal side effects. Numerous animal experiments point out that several indications can be addressed with positive modulators of GABA(B) receptors, such as depression, anxiety, schizophrenia, neuropathic and chronic pain and treatment of craving for drugs of abuse, such as alcohol, cocaine and nicotine. Peripherally acting compounds may be valuable drugs for the treatment of gastroesophageal reflux disease and irritable bowel syndrome. An overview on 19 patents in this field, of the different scaffolds for positive modulators of GABA(B) receptors and of the major players in the field. The search for subtype selective benzodiazepine receptor ligands has proved to be extremely difficult. Positive modulators of GABA(B) receptors may provide novel anxiolytic drugs...Continue Reading

References

Jan 1, 1979·Journal of Medicinal Chemistry·L H Sternbach
Mar 25, 2004·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Cedric MombereauJohn F Cryan
Sep 29, 2004·Biochemical Pharmacology·Andrés CouveMenelas N Pangalos
Apr 21, 2005·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·David A SlatteryJohn F Cryan
Apr 6, 2006·Journal of Receptor and Signal Transduction Research·Thue W Schwartz, Birgitte Holst
May 20, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Loic LhuillierKlemens Kaupmann
Jul 17, 2007·Trends in Pharmacological Sciences·Thue W Schwartz, Birgitte Holst
Sep 22, 2007·Bioorganic & Medicinal Chemistry Letters·Sébastien GueryWolfgang Froestl
Sep 27, 2007·CNS Drug Reviews·C L Adams, A J Lawrence
Sep 1, 2007·Current Neuropharmacology·Jean-Philippe Pin, Laurent Prézeau

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Citations

Mar 25, 2011·Future Medicinal Chemistry·Wolfgang Froestl
Mar 2, 2016·Advanced Drug Delivery Reviews·Christel A S BergströmChristopher J H Porter
Nov 29, 2011·Chemistry & Biology·David E GloriamHans Bräuner-Osborne

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