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Potent and Metabolically Stable Agonists for Protease-Activated Receptor-2: Evaluation of Activity in Multiple Assay Systems in Vitro and in Vivo
It is demonstrated that substitution of the N-terminal serine with a furoyl group in native PAR-2-activating peptides dramatically enhances the agonistic activity and decreases degradation by aminopeptidase, leading to development of 2f-LIGRL-NH2, the most potent peptide. Expand
Species Difference in the Inhibitory Effect of Nonsteroidal Anti-Inflammatory Drugs on the Uptake of Methotrexate by Human Kidney Slices
Inhibition of renal uptake (via OAT3) and efflux processes (via MRP2 and MRP4) explains the possible sites of drug-drug interaction for methotrexate with probenecid and some NSAIDs, including their glucuronides. Expand
Comparative evaluation of 12 immature citrus fruit extracts for the inhibition of cytochrome P450 isoform activities.
Results, providing comparative information on the inhibitory effects of citrus extracts on CYP isoforms, suggest that citrus extracts containing high levels of narirutin and hesperidin and lower levels of furanocoumarins such as C. unshiu are favorable as antiallergic functional ingredients. Expand
Transfollicular Drug Delivery: Penetration of Drugs Through Human Scalp Skin and Comparison of Penetration Between Scalp and Abdominal Skins In Vitro
Results indicate that the drug delivery through the scalp skin will offer an available delivery means for drugs, particularly for hydrophilic drugs. Expand
Pharmacokinetic drug interactions between ampiroxicam and sulfaphenazole in rats.
The results suggest that SP does not significantly affect the pharmacokinetics of AM and PX in rats, and the Pharmacokinetic drug interaction between both drugs in man may not always be ignored. Expand
Pharmacological studies of FUT-175, nafamostat mesilate. V. Effects on the pancreatic enzymes and experimental acute pancreatitis in rats.
Data strongly support that FUT-175 is clinically useful in the therapy of acute pancreatitis and reduces the mortality of rats in the experimental acute pancreas in a dose-dependent manner. Expand
Effect of various enhancers on transdermal penetration of indomethacin and urea, and relationship between penetration parameters and enhancement factors.
In vitro permeation experiments with hairless rat skin unequivocally revealed that the enhancers varied in abilities to enhance the fluxes of both agents, but N-methyl-2-pyrrolidone, N,N-diethyl-m-tolamide, and oleyl oleate were less effective acclerants. Expand
Application of a Physiologically Based Pharmacokinetic Model Informed by a Top-Down Approach for the Prediction of Pharmacokinetics in Chronic Kidney Disease Patients
The developed PBPK model with information on SFs would accelerate translational research in drug development by predicting pharmacokinetics in CKD patients by providing good predictability for plasma concentration. Expand
Pharmacokinetics and metabolism of metoprolol and propranolol in the female DA and female Wistar rat: the female DA rat is not always an animal model for poor metabolizers of CYP2D6.
  • H. Komura, M. Iwaki
  • Biology, Medicine
  • Journal of pharmaceutical sciences
  • 1 February 2005
The larger strain difference in the AUCs of propranolol was proved by the in vitro kinetic parameters, implying that DA rats do not always reflect the polymorphic profiles in humans. Expand
Species differences in in vitro and in vivo small intestinal metabolism of CYP3A substrates.
In vivo assessment of cyclosporine, midazolam, nifedipine, tacrolimus, and verapamil has been reported in various species including the human, and the monkey might be an appropriate animal model for evaluating small intestinal first-pass metabolism of CYP3A substrates. Expand