• Publications
  • Influence
[Opioid agonists and antagonists, opioid receptors].
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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
  • Yulin Wang, Kang Tang, +7 authors L. Liu-Chen
  • Chemistry, Medicine
  • Journal of Pharmacology and Experimental…
  • 1 January 2005
Salvinorin A, TRK-820 (17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl) acrylamido]morphinan hydrochloride), and 3FLB (diethylExpand
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  • PDF
Quantitative NMR spectroscopy in pharmaceutical applications.
  • U. Holzgrabe
  • Chemistry, Medicine
  • Progress in nuclear magnetic resonance…
  • 1 August 2010
2010 Elsevier B.V. All rights reserved.
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The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling
Seven transmembrane helical receptors (7TMRs) modulate cell function via different types of G proteins, often in a ligand-specific manner. Class A 7TMRs harbour allosteric vestibules in the entranceExpand
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Penetration of antibacterials into bone: pharmacokinetic, pharmacodynamic and bioanalytical considerations.
Antibacterials play a key role in the treatment of bone infections and appropriate surgical prophylaxis. The rate and extent of penetration of antimicrobials into bone has been assessed and shown toExpand
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Allosteric ligands for G protein‐coupled receptors: A novel strategy with attractive therapeutic opportunities
Allosteric receptor ligands bind to a recognition site that is distinct from the binding site of the endogenous messenger molecule. As a consequence, allosteric agents may attach to receptors thatExpand
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Penetration of Antibacterials into Bone
Antibacterials play a key role in the treatment of bone infections and appropriate surgical prophylaxis. The rate and extent of penetration of antimicrobials into bone has been assessed and shown toExpand
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Analytical challenges in drug counterfeiting and falsification-The NMR approach.
Counterfeiting of products is a global problem. As long as clothes, clocks, leather wear, etc. are faked there is no danger, but when it comes to drugs, counterfeiting can be life-threatening. In theExpand
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Inhibition of cytochrome P450 3A4 by extracts and kavalactones of Piper methysticum (Kava-Kava).
Inhibitors of cytochrome P450 3A4 (CYP3A4) were identified in crude extracts from the rhizomes of Piper methysticum G. Forst. (Kava-Kava) using bioassay-guided fractionation. After preliminaryExpand
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Dynamic ligand binding dictates partial agonism at a G protein-coupled receptor.
We present a new concept of partial agonism at G protein-coupled receptors. We demonstrate the coexistence of two functionally distinct populations of the muscarinic M2 receptor stabilized by oneExpand
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