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Validation of a method for localised microinjection of drugs into thalamic subregions in rats for epilepsy pharmacological studies
OBJECTIVES To validate a method for the chronic implantation of micro-cannulae to examine the effect of drug administration to two small brain regions critical to the control of generalised seizures,Expand
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Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients
Significance Peptides are valuable leads for drug development, offering advantages over other molecular classes. Specifically, they can bind potently and selectively to drug targets, includingExpand
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Antagonism of Protease-Activated Receptor 2 Protects against Experimental Colitis
Many trypsin-like serine proteases such as β-tryptase are involved in the pathogenesis of colitis and inflammatory bowel diseases. Inhibitors of individual proteases show limited efficacy in treatingExpand
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Protease-activated receptor-2 regulates trypsin expression in the brain and protects against seizures and epileptogenesis
Protease-activated receptor-2 (PAR(2)), primarily involved in inflammation, is highly expressed in limbic regions of the brain such as the hippocampus. Although extracellular proteolysis is involvedExpand
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Cyclic Penta- and Hexaleucine Peptides without N-Methylation Are Orally Absorbed.
Development of peptide-based drugs has been severely limited by lack of oral bioavailability with less than a handful of peptides being truly orally bioavailable, mainly cyclic peptides with N-methylExpand
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Action potential afterdepolarization mediated by a Ca2+-activated cation conductance in myenteric AH neurons
We investigated the nature of afterdepolarizing potentials in AH neurons from the guinea-pig duodenum using whole-cell patch-clamp recordings in intact myenteric ganglia. Afterdepolarizing potentialsExpand
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Improving on nature: making a cyclic heptapeptide orally bioavailable.
The use of peptides in medicine is limited by low membrane permeability, metabolic instability, high clearance, and negligible oral bioavailability. The prediction of oral bioavailability of drugsExpand
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Diet‐induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism
  • J. Lim, A. Iyer, +6 authors D. Fairlie
  • Medicine, Biology
  • FASEB journal : official publication of the…
  • 1 November 2013
Excessive uptake of fatty acids and glucose by adipose tissue triggers adipocyte dysfunction and infiltration of immune cells. Altered metabolic homeostasis in adipose tissue promotes insulinExpand
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Differential Anti-inflammatory Activity of HDAC Inhibitors in Human Macrophages and Rat Arthritis
Vorinostat and other inhibitors of different histone deacetylase (HDAC) enzymes are currently being sought to modulate a variety of human conditions, including chronic inflammatory diseases. SomeExpand
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Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a
Complement C3a is an important protein in innate and adaptive immunity, but its specific roles in vivo remain uncertain because C3a degrades rapidly to form the C3a-desArg protein, which does notExpand
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