S Urwyler

Summary

Affiliation: Novartis Institutes for BioMedical Research

Publications

  1. ncbi Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501
    S Urwyler
    Novartis Pharma AG, TA Nervous System, Basel, Switzerland
    Mol Pharmacol 60:963-71. 2001
  2. ncbi N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland
    J Pharmacol Exp Ther 307:322-30. 2003
  3. ncbi Selected amino acids, dipeptides and arylalkylamine derivatives do not act as allosteric modulators at GABAB receptors
    Stephan Urwyler
    Neuroscience Research, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH 4002 Basel, Switzerland
    Eur J Pharmacol 483:147-53. 2004
  4. ncbi Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Neuroscience, WKL 125 11 03, CH 4002 Basel, Switzerland
    Neuropharmacology 48:343-53. 2005
  5. ncbi Changes in the properties of allosteric and orthosteric GABAB receptor ligands after a continuous, desensitizing agonist pretreatment
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    Eur J Pharmacol 603:37-41. 2009
  6. ncbi Receptor activation involving positive allosteric modulation, unlike full agonism, does not result in GABAB receptor desensitization
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    Neuropharmacology 55:1293-9. 2008
  7. ncbi Novel N-methyl-D-aspartate receptor antagonists: a review of compounds patented since 2006
    Manuel Koller
    Novartis Institutes for BioMedical Research, Global Discovery Chemistry, Basel, Switzerland
    Expert Opin Ther Pat 20:1683-702. 2010
  8. ncbi The positive allosteric modulator GS39783 enhances GABA(B) receptor-mediated inhibition of cyclic AMP formation in rat striatum in vivo
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    J Neurochem 96:1416-22. 2006
  9. ncbi Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Neuroscience, 4056 Basel, Switzerland
    J Med Chem 52:5093-107. 2009
  10. ncbi Roles of GABAB receptor subtypes in presynaptic auto- and heteroreceptor function regulating GABA and glutamate release
    Peter C Waldmeier
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    J Neural Transm 115:1401-11. 2008

Collaborators

Detail Information

Publications12

  1. ncbi Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501
    S Urwyler
    Novartis Pharma AG, TA Nervous System, Basel, Switzerland
    Mol Pharmacol 60:963-71. 2001
    ..This first demonstration of positive allosteric modulation at GABA(B) receptors may represent a novel means of therapeutic interference with the GABA-ergic system...
  2. ncbi N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland
    J Pharmacol Exp Ther 307:322-30. 2003
    ..This effect is reversed by the competitive GABA(B) receptor antagonist CGP55845A and is produced most likely by enhancing the effect of synaptically released GABA at presynaptic GABA(B) receptors...
  3. ncbi Selected amino acids, dipeptides and arylalkylamine derivatives do not act as allosteric modulators at GABAB receptors
    Stephan Urwyler
    Neuroscience Research, Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH 4002 Basel, Switzerland
    Eur J Pharmacol 483:147-53. 2004
    ..It is concluded that the arylalkylamines, amino acids and dipeptides tested do not act as allosteric modulators at native and recombinant GABA(B) receptors...
  4. ncbi Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Neuroscience, WKL 125 11 03, CH 4002 Basel, Switzerland
    Neuropharmacology 48:343-53. 2005
    ..These results show that the intrinsic properties of orthosteric ligands are highly dependent on the characteristics of the assay system used and that allosteric modulators are useful tools for elucidating these properties...
  5. ncbi Changes in the properties of allosteric and orthosteric GABAB receptor ligands after a continuous, desensitizing agonist pretreatment
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    Eur J Pharmacol 603:37-41. 2009
    ....
  6. ncbi Receptor activation involving positive allosteric modulation, unlike full agonism, does not result in GABAB receptor desensitization
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    Neuropharmacology 55:1293-9. 2008
    ..In summary, our results conform to predictions that positive allosteric modulators have less propensity for the development of tolerance due to receptor desensitization than classical agonists...
  7. ncbi Novel N-methyl-D-aspartate receptor antagonists: a review of compounds patented since 2006
    Manuel Koller
    Novartis Institutes for BioMedical Research, Global Discovery Chemistry, Basel, Switzerland
    Expert Opin Ther Pat 20:1683-702. 2010
    ....
  8. ncbi The positive allosteric modulator GS39783 enhances GABA(B) receptor-mediated inhibition of cyclic AMP formation in rat striatum in vivo
    Tina Gjoni
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    J Neurochem 96:1416-22. 2006
    ..To our knowledge, these results provide the first biochemical demonstration of in vivo activity of a G protein-coupled receptor-positive allosteric modulator...
  9. ncbi Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex
    Stephan Urwyler
    Novartis Institutes for BioMedical Research, Neuroscience, 4056 Basel, Switzerland
    J Med Chem 52:5093-107. 2009
    ....
  10. ncbi Roles of GABAB receptor subtypes in presynaptic auto- and heteroreceptor function regulating GABA and glutamate release
    Peter C Waldmeier
    Novartis Institutes for BioMedical Research, Neuroscience, Basel, Switzerland
    J Neural Transm 115:1401-11. 2008
    ..Our data suggest that functional GABA B heteroreceptors regulating glutamate release are predominantly, but not exclusively composed of GABA B(1a) and GABA B(2) subunits...
  11. ncbi ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies
    Samuel Hintermann
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    Bioorg Med Chem 15:903-14. 2007
    ....
  12. ncbi Survival signaling and selective neuroprotection through glutamatergic transmission
    Ben A Bahr
    Department of Pharmaceutical Sciences and the Neurosciences Program, Center for Drug Discovery, University of Connecticut, Storrs, Connecticut, USA
    Exp Neurol 174:37-47. 2002
    ..The results indicate that glutamatergic communication is important for cellular maintenance and that AMPA receptors activate survival signals to counterpoise their own excitotoxic potential...