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Quantitative Evaluation of the Impact of Active Efflux by P-Glycoprotein and Breast Cancer Resistance Protein at the Blood-Brain Barrier on the Predictability of the Unbound Concentrations of Drugs
Cu,CSF of non-P-gp and non-Bcrp substrates can be a reliable surrogate of Cu,brain for lipophilic compounds and decreases along with the net transport activities by P-glycoprotein and Bcrp at the BBB. Expand
Putrescine N-Methyltransferase in Cultured Roots of Hyoscyamus albus: n-Butylamine as a Potent Inhibitor of the Transferase both in Vitro and in Vivo.
PMT was partially purified and characterized from cultured roots of Hyoscyamus albus that contain hyoscyamine as the main alkaloid and Monoamines were good competitive inhibitors of PMT, among which n-butylamine, cyclohexylamines, and exo-2-aminonorbornane were most inhibitory. Expand
Pharmacokinetic interaction study of sulphasalazine in healthy subjects and the impact of curcumin as an in vivo inhibitor of BCRP
The effect of curcumin, the principalCurcuminoid of turmeric, on oral bioavailability of microdoses and therapeutic doses of sulphasalazine in humans is examined. Expand
Oseltamivir (Tamiflu) Efflux Transport at the Blood-Brain Barrier via P-Glycoprotein
Results show that oseltamivir, but not Ro 64–0802, is a substrate of P-gp, and this may in turn account for the central nervous system effects of oselTAMivir observed in some patients. Expand
Modulation of intestinal P-glycoprotein function by cremophor EL and other surfactants by an in vitro diffusion chamber method using the isolated rat intestinal membranes.
It is indicated that nonionic surfactants including Cremophor EL and Tween 80 may be useful pharmaceutical excipients for inhibiting the function of P- gp, thereby increasing the intestinal absorption of various drugs, which are secreted by a P-gp-mediated efflux system in the intestine. Expand
FR167653, a p38 mitogen-activated protein kinase inhibitor, prevents Helicobacter pylori-induced gastritis in Mongolian gerbils.
The results indicate that p38 kinase plays a crucial role in H. pylori-induced gastritis in Mongolian gerbils and that FR167653 is a p38 Kinase-selective inhibitor without affecting COX activity. Expand
Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies.
It is suggested that PEGs and their derivatives are useful excipients to inhibit the function of intestinal P-gp, thereby improving the intestinal absorption of P- gp substrates, which are secreted by a P-GP-mediated efflux system. Expand
P-glycoprotein Restricts the Penetration of Oseltamivir Across the Blood-Brain Barrier
The results suggest that P-gp limits the brain uptake of oseltamivir at the blood-brain barrier (BBB) and that Ro 64-0802 itself barely crosses the BBB. Expand
What kinds of substrates show P-glycoprotein-dependent intestinal absorption? Comparison of verapamil with vinblastine.
The influence of P-glycoprotein (P-gp) on intestinal absorption of drugs was investigated by comparison of the uptakes of two P-gp substrates, verapamil and vinblastine, using intestinal segments ofExpand
Effects of Various Protease Inhibitors on the Intestinal Absorption and Degradation of Insulin in Rats
It was found that the reduction in the proteolytic rate of insulin was related to the decrease in plasma glucose concentration by these protease inhibitors in the large intestine. Expand