Efflux transport systems for drugs at the blood–brain barrier and blood–cerebrospinal fluid barrier (Part 1)

Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.

1987 • 2,788 citations

Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs

1994 • 2,255 citations

Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites.

1989 • 1,744 citations

P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs.

1996 • 1,268 citations

Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A.

1995 • 1,109 citations

The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.

1998 • 1,058 citations

Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins

1997 • 934 citations

P-Glycoprotein, a gatekeeper in the blood–brain barrier

1999 • 918 citations

Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability

1980 • 799 citations

Choroid plexus epithelial expression of MDR 1 P glycoprotein and multidrug resistance-associated protein contribute to the blood–cerebrospinal-fluid drug-permeability barrier

1999 • 529 citations

Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs

2000 • 473 citations

Cellular and molecular aspects of drug transport in the kidney

2000 • 445 citations

The Multidrug Resistance Protein 5 Functions as an ATP-dependent Export Pump for Cyclic Nucleotides

2000 • 438 citations

Increased sensitivity to anticancer drugs and decreased inflammatory response in mice lacking the multidrug resistance-associated protein

1997 • 432 citations

Structural, mechanistic and clinical aspects of MRP1

1999 • 408 citations

Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier.

2000 • 399 citations

Hepatobiliary secretion of organic compounds; molecular mechanisms of membrane transport

1995 • 385 citations

Biology of the multidrug resistance-associated protein, MRP

1996 • 367 citations

Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier

2000 • 358 citations

Functional involvement of P-glycoprotein in blood-brain barrier.

1992 • 352 citations

Substrate specificity of sinusoidal bile acid and organic anion uptake systems in rat and human liver

1997 • 352 citations

The multispecific organic anion transporter (OAT) family

2000 • 315 citations

Placental P-glycoprotein deficiency enhances susceptibility to chemically induced birth defects in mice

1998 • 308 citations

Molecular aspects of hepatobiliary transport

1997 • 304 citations

Localization of the Organic Anion Transporting Polypeptide 2 (Oatp2) in Capillary Endothelium and Choroid Plexus Epithelium of Rat Brain

1999 • 300 citations

Structure of renal organic anion and cation transporters

2000 • 296 citations

P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells

1992 • 288 citations

Intestinal secretion of drugs. The role of P-glycoprotein and related drug efflux systems in limiting oral drug absorption

1997 • 287 citations

Transport of small molecules through the blood-brain barrier: biology and methodology

1995 • 265 citations

Expression of various multidrug resistance-associated protein (MRP) homologues in brain microvessel endothelial cells

2000 • 233 citations

Brain efflux index as a novel method of analyzing efflux transport at the blood-brain barrier.

1996 • 225 citations

Localization and function of the organic anion–transporting polypeptide Oatp2 in rat liver

1999 • 209 citations

P-Glycoprotein Deficiency in a Subpopulation of CF-1 Mice Enhances Avermectin-Induced Neurotoxicity

1997 • 203 citations

Expression of Multidrug Resistance-Associated Protein (MRP) in Brain Microvessel Endothelial Cells

1998 • 202 citations

Multidrug Resistance Protein 1 Protects the Oropharyngeal Mucosal Layer and the Testicular Tubules against Drug-induced Damage

1998 • 200 citations

Multidrug resistance and the role of P-glycoprotein knockout mice

1995 • 199 citations

Development of anIn SituMouse Brain Perfusion Model and its Application tomdr1aP-Glycoprotein-Deficient Mice

2000 • 196 citations

Complete in vivo reversal of P‐glycoprotein pump function in the blood‐brain barrier visualized with positron emission tomography

1998 • 182 citations

Demonstration of a Coupled Metabolism–Efflux Process at the Choroid Plexus as a Mechanism of Brain Protection Toward Xenobiotics

1999 • 180 citations

Altered Pharmacokinetics of Vinblastine in Mdr1a P-glycoprotein-Deficient Mice

1996 • 175 citations

Localization of Drug‐Metabolizing Enzyme Activities to Blood‐Brain Interfaces and Circumventricular Organs

1994 • 174 citations

Carrier-mediated or specialized transport of drugs across the blood–brain barrier

1999 • 164 citations

Brain Microvascular and Astrocyte Localization of P‐Glycoprotein

1997 • 146 citations

Pharmacological Characterization of the Murine and Human Orthologs of Multidrug-Resistance Protein in Transfected Human Embryonic Kidney Cells

1997 • 143 citations

In vivo evidence for ATP-dependent and P-glycoprotein-mediated transport of cyclosporin A at the blood-brain barrier

1994 • 141 citations

99mTc-sestamibi is a substrate for P-glycoprotein and the multidrug resistance-associated protein

1998 • 141 citations

The choroid plexus epithelium is the site of the organic anion transport protein in the brain

1997 • 140 citations

P-Glycoprotein mediates the efflux of quinidine across the blood-brain barrier.

1997 • 140 citations

Multidrug Resistance‐Related Transport Proteins in Isolated Human Brain Microvessels and in Cells Cultured from These Isolates

1998 • 139 citations

In vivo and in vitro evidence for ATP-dependency of P-glycoprotein-mediated efflux of doxorubicin at the blood-brain barrier

1995 • 132 citations

Identification of a P-Glycoprotein-Deficient Subpopulation in the CF-1 Mouse Strain Using a Restriction Fragment Length Polymorphism

1997 • 123 citations

The Role of P-Glycoprotein and Canalicular Multispecific Organic Anion Transporter in the Hepatobiliary Excretion of Drugs

1998 • 118 citations

P-glycoprotein-dependent disposition kinetics of tacrolimus: studies in mdr1a knockout mice.

1999 • 113 citations

Role of blood‐brain barrier P‐glycoprotein in limiting brain accumulation and sedative side‐effects of asimadoline, a peripherally acting analgaesic drug

1999 • 106 citations

Kinetic evidence suggesting that the multidrug transporter differentially handles influx and efflux of its substrates.

1994 • 103 citations

BBB transport and P-glycoprotein functionality using MDR1A (-/-) and wild-type mice. Total brain versus microdialysis concentration profiles of rhodamine-123.

1998 • 103 citations

In vivo evidence for carrier-mediated efflux transport of 3'-azido-3'-deoxythymidine and 2',3'-dideoxyinosine across the blood-brain barrier via a probenecid-sensitive transport system.

1997 • 98 citations

Immunohistochemical detection of multidrug resistance protein in human lung cancer and normal lung.

1998 • 98 citations

Dexamethasone Regulation of P‐Glycoprotein Activity in an Immortalized Rat Brain Endothelial Cell Line, GPNT

1999 • 98 citations

Specialized Localization of P‐Glycoprotein Recognized by MRK 16 Monoclonal Antibody in Endothelial Cells of the Brain and the Spinal Cord

1990 • 97 citations

Functional Reconstitution of Substrate Transport by Purified Multidrug Resistance Protein MRP1 (ABCC1) in Phospholipid Vesicles

2000 • 95 citations

Characterization of efflux transport of organic anions in a mouse brain capillary endothelial cell line.

1998 • 94 citations

The blood–brain barrier efflux transporters as a detoxifying system for the brain

1999 • 92 citations

Role of efflux transport across the blood-brain barrier and blood-cerebrospinal fluid barrier on the disposition of xenobiotics in the central nervous system

1997 • 88 citations

Limited distribution of new quinolone antibacterial agents into brain caused by multiple efflux transporters at the blood-brain barrier.

2000 • 84 citations

Mechanism of Organic Anion Transport across the Apical Membrane of Choroid Plexus

1999 • 80 citations

Comparisons of P‐glycoprotein expression in isolated rat brain microvessels and in primary cultures of endothelial cells derived from microvasculature of rat brain, epididymal fat pad and from aorta

1995 • 80 citations

Transport of cyclosporin A across the brain capillary endothelial cell monolayer by P-glycoprotein

1994 • 78 citations

Transepithelial transport of organic anions across the choroid plexus: possible involvement of organic anion transporter and multidrug resistance-associated protein.

1999 • 76 citations

Efflux of taurocholic acid across the blood-brain barrier: interaction with cyclic peptides.

1998 • 66 citations

Selective brain to blood efflux transport of para-aminohippuric acid across the blood-brain barrier: in vivo evidence by use of the brain efflux index method.

1997 • 64 citations

Active transport properties of porcine choroid plexus cells in culture

1998 • 56 citations

Drug Transport in the Mammalian Central Nervous System: Multiple Complex Systems

2000 • 54 citations

Modulation of doxorubicin concentration by cyclosporin A in brain and testicular barrier tissues expressing P-glycoprotein in rats.

1998 • 49 citations

High-affinity efflux transport system for glutathione conjugates on the luminal membrane of a mouse brain capillary endothelial cell line (MBEC4).

1999 • 44 citations

Efflux transport of a new quinolone antibacterial agent, HSR-903, across the blood-brain barrier.

1999 • 41 citations

In Vivo Study of the Elimination from Rat Brain of an Intracerebrally Formed Xenobiotic Metabolite, 1‐Naphthyl‐β‐D‐Glucuronide

1991 • 40 citations

Regulation of initial vinblastine influx by P-glycoprotein

1993 • 40 citations

Effect of P-glycoprotein modulation with cyclosporin A on cerebrospinal fluid penetration of doxorubicin in non-human primates

2000 • 36 citations

Saturable accumulation of the anionic herbicide, 2,4-dichlorophenoxyacetic acid (2,4-D), by rabbit choroid plexus: early developmental origin and interaction with salicylates.

1983 • 34 citations

Saturable efflux of the peptides RC-160 and Tyr-MIF-1 by different parts of the blood-brain barrier

1994 • 33 citations

Characterization of the transport properties of a quinolone antibiotic, fleroxacin, in rat choroid plexus.

1996 • 22 citations

Transport of cefodizime, a novel third generation cephalosporin antibiotic, in isolated rat choroid plexus.

1989 • 22 citations

Effect of the Mdr1a P-glycoprotein gene disruption on the tissue distribution of SDZ PSC 833, a multidrug resistance-reversing agent, in mice.

1998 • 17 citations

Renal secretion of xenobiotics mediated by P-glycoprotein: Importance to renal function in health and exploitation for targeted drug delivery to epithelial cysts in polycystic kidney disease

1997 • 9 citations