Results 301 to 310 of about 20,489,060 (330)

Evaluation of the Impact of P-Glycoprotein (P-gp) Drug Efflux Transporter Blockade on the Systemic and Ocular Disposition of P-gp Substrate

Journal of Ocular Pharmacology and Therapeutics, 2008
The impact of P-glycoprotein (P-gp) blockade on the intravenous (i.v.) pharmacokinetics of rhodamine-123 (Rho-123), and the subsequent effect on its disposition in ocular and nonocular tissues, was studied by using rabbits.Three (3) control rabbits received only an i.v. bolus dose of Rho-123 (1.52 mg/kg).
Srinivasan, Senthilkumari, Thirumurthy, Velpandian, Nihar R, Biswas, Narayanan, Sonali, Supriyo, Ghose   +4 more
openaire   +2 more sources

Estradiol and Progesterone-Mediated Regulation of P-gp in P-gp Overexpressing Cells (NCI-ADR-RES) and Placental Cells (JAR)

Molecular Pharmaceutics, 2009
The effect of progesterone and estrogen treatment on the expression and function of P-glycoprotein (P-gp) was evaluated in JAR cells and a P-gp overexpressing cell line, NCI-ADR-RES. Western blot analysis and real-time Q-PCR were used to evaluate P-gp protein and MDR1 mRNA expression respectively in the cells following incubation with progesterone (P4)
Lisa D, Coles, Insong J, Lee, Pamela J, Voulalas, Natalie D, Eddington   +3 more
openaire   +2 more sources

Drug Efflux Transporters: P-gp and BCRP

2021
The efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) play important roles in protecting tissues from potentially harmful xenobiotic substances, mainly by virtue of their location in the intestinal epithelium and in the blood–brain barrier.
Peter Bungay, Sharan Bagal
openaire   +1 more source

Evaluation of the Role of P-glycoprotein (P-gp)-Mediated Efflux in the Intestinal Absorption of Common Substrates with Elacridar, a P-gp Inhibitor, in Rats

European Journal of Drug Metabolism and Pharmacokinetics, 2020
P-glycoprotein (P-gp) has been shown previously to contribute to the intestinal absorption of verapamil, diltiazem, tacrolimus, colchicine and indinavir in situ; however, its contribution in vivo is unknown. The present study aimed to evaluate the in vivo involvement of P-gp using elacridar as its inhibitor to distinguish the contribution of P-gp from ...
Kei Suzuki, Kazuhiro Taniyama, Takao Aoyama, Yoshiaki Watanabe   +3 more
openaire   +2 more sources

Regulation of hepatic P-gp expression and activity by genistein in rats

Archives of Toxicology, 2020
P-glycoprotein (P-gp) is an ABC transporter exhibiting high pharmacotoxicological relevance by extruding a wide range of cytotoxic compounds out of the cells. Previously, we demonstrated that the phytoestrogen genistein (GNT) modulates P-gp expression in hepatocellular carcinoma in vitro.
M. Semeniuk, L. I. Ceré, N. Ciriaci, M. Bucci-Muñoz, S. S. M. Villanueva, A. D. Mottino, V. A. Catania, J. P. Rigalli, María Laura Ruiz   +8 more
openaire   +4 more sources

FUNCTIONAL ASSESSMENT OF MULTIPLE P-GLYCOPROTEIN (P-GP) PROBE SUBSTRATES: INFLUENCE OF CELL LINE AND MODULATOR CONCENTRATION ON P-GP ACTIVITY

Drug Metabolism and Disposition, 2005
Compounds known to modulate P-glycoprotein (P-gp) activity were evaluated in cell monolayers expressing P-gp for their effects on the secretory transport of P-gp substrates paclitaxel, vinblastine, and digoxin. Paclitaxel has been proposed to selectively interact with a binding site on P-gp that is distinct from the vinblastine and digoxin-binding site.
Mitchell E, Taub, Lalitha, Podila, Diane, Ely, Iliana, Almeida   +3 more
openaire   +2 more sources

The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib

Investigational New Drugs, 2008
Imatinib is transported by P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP), however, the exact impact of these transporters on absorption, distribution, metabolism and excretion (ADME) of imatinib is not fully understood due to incomplete data.
Oostendorp, R.L., Buckle, T., Beijnen, J.H., van Tellingen, O., Schellens, J.H.M.   +4 more
openaire   +3 more sources

Model Analysis of the Concentration-Dependent Permeability of P-gp Substrates

Pharmaceutical Research, 2010
Recently, it was reported that the apparent Michaelis-Menten constant (Km(app)) of a P-glycoprotein (P-gp) substrate, defined for the extracellular substrate concentration, increases as the P-gp expression level in the cell increases. By its nature, the Km value should not depend on the level of P-gp expression.
Tatsuhiko, Tachibana, Satoshi, Kitamura, Motohiro, Kato, Tetsuya, Mitsui, Yoshiyuki, Shirasaka, Shinji, Yamashita, Yuichi, Sugiyama   +6 more
openaire   +2 more sources

Study of Oxidized Lipids as Endogenous Substrates of P-gp (ABCB1)

Drug Metabolism Letters, 2008
We studied endogenous substrates for P-glycoprotein (P-gp) in an oxidative reaction mixture of ceramides, phospholipids, sphingolipids, or GM1-gangliosides (GM1-G). Extracts from the reaction mixture of galactocerebrosides (GalCer), sphingomyelin (SM) , lactocerebrosides (LactoCer), and asolectine (AS) with 0.3% hydrogen peroxide exhibited significant ...
Masatoshi, Masuda, Emi, Nakai, Takaharu, Mizutani   +2 more
openaire   +2 more sources

Effect of Ultrasound-Induced Hyperthermia on Cellular Uptake of P-gp Substrate and Non-P-gp Substrate in MDR Cells

Journal of Korean Pharmaceutical Sciences, 2007
A previous report recently demonstrated that ultrasound-induced hyperthermia (USHT:0.4 watts (W)/ at ) could increase cellular uptake of P-glycoprotein (P-gp) substrates in P-gp expressing cancer cell lines. Since P-gp plays a major role in limiting drug permeability in the multi-drug resistant (MDR) cells, studies were conducted to elucidate the ...
openaire   +1 more source