• Publications
  • Influence
Quantitative NMR spectroscopy in pharmaceutical applications.
  • U. Holzgrabe
  • Geography, Chemistry
    Progress in nuclear magnetic resonance…
  • 1 August 2010
Comparison of Pharmacological Activities of Three Distinct κ Ligands (Salvinorin A, TRK-820 and 3FLB) on κ Opioid Receptors in Vitro and Their Antipruritic and Antinociceptive Activities in Vivo
TLDR
In vitro pharmacological activities on receptors expressed in Chinese hamster ovary cells and in vivo antiscratch and antinociceptive activities in mice are investigated and salvinorin A, TRK-820, and 3FLB caused internalization of the human KOR in a dose-dependent manner.
Penetration of antibacterials into bone: pharmacokinetic, pharmacodynamic and bioanalytical considerations.
TLDR
Established and new sample preparation and analytical methods to measure bone concentrations and the extent and rate of bone penetration of antibacterials, and the design, evaluation and reporting techniques of pharmacokinetic studies ofBone penetration studies are compared.
The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling
TLDR
These findings reveal for the first time that a 7TMR's allosteric vestibule controls the extent of receptor movement to govern a hierarchical order of G-protein coupling.
Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor
TLDR
This work hypothesized that iperoxo is a ‘superagonist’, which may have higher efficacy for receptor activation than the physiological agonist.
Atypical Muscarinic Allosteric Modulation: Cooperativity between Modulators and Their Atypical Binding Topology in Muscarinic M2 and M2/M5 Chimeric Receptors
TLDR
The atypical actions of tacrine and Duo3 involve different modes of receptor interaction, but their sites of attachment seem to be the “common” allosteric binding domain at the entrance to the orthosteric ligand binding pocket of the M2-receptor.
Penetration of Antibacterials into Bone
TLDR
Established and new sample preparation and analytical methods to measure bone concentrations and the extent and rate of bone penetration of antibacterials are compared, with a focus on studies conducted between 1998 and 2007.
Analytical challenges in drug counterfeiting and falsification-The NMR approach.
Allosteric ligands for G protein‐coupled receptors: A novel strategy with attractive therapeutic opportunities
TLDR
A suitable exploitation of allosteric recognition sites as alternative molecular targets could pave the way to a drug discovery paradigm different from those aimed at mimicking or blocking the effects of endogenous (orthosteric) receptor activators.
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