Drug interactions at the blood-brain barrier: Fact or fantasy?☆

A default mode of brain function

2001 • 11,745 citations

Multidrug resistance in cancer: role of ATP–dependent transporters

2002 • 5,195 citations

Astrocyte–endothelial interactions at the blood–brain barrier

2005 • 4,950 citations

BIOCHEMISTRY OF MULTIDRUG RESISTANCE MEDIATED BY THE MULTIDRUG TRANSPORTER

1993 • 3,515 citations

Targeting multidrug resistance in cancer

2006 • 3,410 citations

A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants

1976 • 3,228 citations

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

1987 • 2,788 citations

FINE STRUCTURAL LOCALIZATION OF A BLOOD-BRAIN BARRIER TO EXOGENOUS PEROXIDASE

1967 • 2,534 citations

The Blood-Brain Barrier/Neurovascular Unit in Health and Disease

2005 • 2,454 citations

JUNCTIONS BETWEEN INTIMATELY APPOSED CELL MEMBRANES IN THE VERTEBRATE BRAIN

1969 • 2,408 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

Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil.

1981 • 1,463 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

Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues.

1990 • 1,063 citations

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

1998 • 1,058 citations

Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties

2004 • 976 citations

Polyspecific Organic Cation Transporters: Structure, Function, Physiological Roles, and Biopharmaceutical Implications

2007 • 959 citations

The ABCs of solute carriers: physiological, pathological and therapeutic implications of human membrane transport proteins

2004 • 940 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

Role of P-Glycoprotein in Pharmacokinetics

2003 • 897 citations

Drug resistance in brain diseases and the role of drug efflux transporters

2005 • 848 citations

Transmembrane Transport of Endo- and Xenobiotics by Mammalian ATP-Binding Cassette Multidrug Resistance Proteins

2006 • 740 citations

Role of Breast Cancer Resistance Protein in the Bioavailability and Fetal Penetration of Topotecan

2000 • 640 citations

Monocarboxylate transporters in the central nervous system: distribution, regulation and function

2005 • 637 citations

EVOLUTION OF THE ATP-BINDING CASSETTE (ABC) TRANSPORTER SUPERFAMILY IN VERTEBRATES

2005 • 614 citations

OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.

1999 • 585 citations

Outwitting the Blood-Brain Barrier for Therapeutic Purposes: Osmotic Opening and Other Means

1998 • 574 citations

Modelling of the blood–brain barrier in drug discovery and development

2007 • 570 citations

Drug transporters in the central nervous system: brain barriers and brain parenchyma considerations.

2001 • 537 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

The SLC22 drug transporter family

2004 • 519 citations

Quantitative Atlas of Membrane Transporter Proteins: Development and Application of a Highly Sensitive Simultaneous LC/MS/MS Method Combined with Novel In-silico Peptide Selection Criteria

2008 • 474 citations

THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL

2004 • 437 citations

Overexpression of Multiple Drug Resistance Genes in Endothelial Cells from Patients with Refractory Epilepsy

2001 • 432 citations

Ivermectin sensitivity in collies is associated with a deletion mutation of the mdr1 gene

2001 • 424 citations

Increased drug delivery to the brain by P-glycoprotein inhibition

2000 • 422 citations

Mrp4 Confers Resistance to Topotecan and Protects the Brain from Chemotherapy

2004 • 407 citations

Localisation of breast cancer resistance protein in microvessel endothelium of human brain

2002 • 405 citations

Isolation of a multispecific organic anion and cardiac glycoside transporter from rat brain

1997 • 396 citations

Inhibition of P-Glycoprotein–Mediated Drug Transport

1999 • 395 citations

Osmotic opening of the blood-brain barrier: principles, mechanism, and therapeutic applications.

2000 • 395 citations

Role of the breast cancer resistance protein (ABCG2) in drug transport

2005 • 394 citations

Transport of Amino Acid-Related Compounds Mediated by L-Type Amino Acid Transporter 1 (LAT1): Insights Into the Mechanisms of Substrate Recognition

2002 • 392 citations

Chemotherapy Delivery Issues in Central Nervous System Malignancy: A Reality Check

2007 • 390 citations

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.

2000 • 384 citations

Expression and immunolocalization of the multidrug resistance proteins, MRP1–MRP6 (ABCC1–ABCC6), in human brain

2004 • 369 citations

Testing of a hypothesis for osmotic opening of the blood-brain barrier

1972 • 366 citations

Pharmacological and Physiological Functions of the Polyspecific Organic Cation Transporters: OCT1, 2, and 3 (SLC22A1-3)

2003 • 364 citations

Modulation of P-Glycoprotein at the Blood-Brain Barrier: Opportunities to Improve Central Nervous System Pharmacotherapy

2008 • 360 citations

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

2000 • 358 citations

Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo

2002 • 358 citations

The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients

2005 • 348 citations

Cisplatin and Oxaliplatin, but Not Carboplatin and Nedaplatin, Are Substrates for Human Organic Cation Transporters (SLC22A1–3 and Multidrug and Toxin Extrusion Family)

2006 • 331 citations

Clinical Pharmacokinetic and Pharmacodynamic Properties of Drugs Used in the Treatment of Parkinson??s Disease

2002 • 327 citations

Use of P-glycoprotein and BCRP inhibitors to improve oral bioavailability and CNS penetration of anticancer drugs

2005 • 318 citations

Expression, Up-Regulation, and Transport Activity of the Multidrug-Resistance Protein Abcg2 at the Mouse Blood-Brain Barrier

2004 • 315 citations

ABC transporters, cytochromes P450 and their main transcription factors: expression at the human blood–brain barrier

2008 • 312 citations

Pharmacokinetic role of L-type amino acid transporters LAT1 and LAT2

2008 • 302 citations

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

1999 • 300 citations

Stimulation of P‐glycoprotein‐mediated drug transport by prazosin and progesterone

1999 • 299 citations

Expression of the Thyroid Hormone Transporters Monocarboxylate Transporter-8 (SLC16A2) and Organic Ion Transporter-14 (SLCO1C1) at the Blood-Brain Barrier

2008 • 290 citations

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

1992 • 288 citations

Pregnane X Receptor Up-Regulation of P-Glycoprotein Expression and Transport Function at the Blood-Brain Barrier

2004 • 287 citations

ABCC Drug Efflux Pumps and Organic Anion Uptake Transporters in Human Gliomas and the Blood-Tumor Barrier

2005 • 286 citations

Impaired Organic Anion Transport in Kidney and Choroid Plexus of Organic Anion Transporter 3 (Oat3 (Slc22a8)) Knockout Mice

2002 • 284 citations

Microvessel Organization and Structure in Experimental Brain Tumors: Microvessel Populations with Distinctive Structural and Functional Properties

1999 • 278 citations

Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833.

1997 • 272 citations

The management of brain edema in brain tumors

2004 • 271 citations

Organic Anion Transporters of the SLC22 Family: Biopharmaceutical, Physiological, and Pathological Roles

2007 • 271 citations

Opiate-induced Analgesia Is Increased and Prolonged in Mice Lacking P-glycoprotein

2000 • 270 citations

Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography

2005 • 268 citations

System L: heteromeric exchangers of large, neutral amino acids involved in directional transport

2003 • 266 citations

Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacodynamics

2004 • 266 citations

P-Glycoprotein and Breast Cancer Resistance Protein: Two Dominant Transporters Working Together in Limiting the Brain Penetration of Topotecan

2007 • 264 citations

IN VITRO P-GLYCOPROTEIN INHIBITION ASSAYS FOR ASSESSMENT OF CLINICAL DRUG INTERACTION POTENTIAL OF NEW DRUG CANDIDATES: A RECOMMENDATION FOR PROBE SUBSTRATES

2006 • 262 citations

The molecular interaction of the high affinity reversal agent XR9576 with P‐glycoprotein

1999 • 258 citations

Increased Permeability of the Blood-Brain Barrier to Chemotherapy in Metastatic Brain Tumors: Establishing a Treatment Paradigm

2007 • 254 citations

Diethylstilbestrol is a potent inhibitor of store-operated channels and capacitative Ca(2+) influx.

2004 • 253 citations

P-glycoprotein is strongly expressed in the luminal membranes of the endothelium of blood vessels in the brain

1997 • 249 citations

Interactions between antiepileptic and chemotherapeutic drugs

2003 • 249 citations

Development of inhibitors of ATP-binding cassette drug transporters – present status and challenges

2008 • 241 citations

Increased penetration of paclitaxel into the brain by inhibition of P-Glycoprotein.

2003 • 238 citations

The structure of the choroid plexus and the physiology of the choroid plexus epithelium

2004 • 235 citations

(Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) Mammalian Nucleoside Transporters

2004 • 235 citations

Considerations in the Use of Cerebrospinal Fluid Pharmacokinetics to Predict Brain Target Concentrations in the Clinical Setting

2002 • 234 citations

Multidrug Resistance Protein MRP2 Contributes to Blood-Brain Barrier Function and Restricts Antiepileptic Drug Activity

2003 • 232 citations

P-Glycoprotein-mediated efflux of phenobarbital, lamotrigine, and felbamate at the blood–brain barrier: evidence from microdialysis experiments in rats

2002 • 230 citations

Multidrug Transporter ABCG2 Prevents Tumor Cell Death Induced by the Epidermal Growth Factor Receptor Inhibitor Iressa (ZD1839, Gefitinib)

2005 • 228 citations

Clinical trials of agents that reverse multidrug resistance. A literature review

1993 • 227 citations

Identification of OATP1B3 as a high-affinity hepatocellular transporter of paclitaxel

2005 • 227 citations

Subcellular localization of transporters along the rat blood–brain barrier and blood–cerebral-spinal fluid barrier by in vivo biotinylation

2008 • 226 citations

P-Glycoprotein Limits the Brain Penetration of Nonsedating but not Sedating H1-Antagonists

2003 • 225 citations

Active efflux across the blood-brain barrier: Role of the solute carrier family

2004 • 224 citations

Limbic seizures induce P-glycoprotein in rodent brain: functional implications for pharmacoresistance.

2002 • 219 citations

The multidrug transporter hypothesis of drug resistance in epilepsy: Proof-of-principle in a rat model of temporal lobe epilepsy

2006 • 218 citations

Role of transporters in drug interactions

2011 • 216 citations

Variable modulation of opioid brain uptake by P-glycoprotein in mice

2003 • 211 citations

Metabolic Drug Interactions

2000 • 208 citations

Sulfation of Thyroid Hormone and Dopamine during Human Development: Ontogeny of Phenol Sulfotransferases and Arylsulfatase in Liver, Lung, and Brain¹

2001 • 204 citations

In Situ Localization of P-glycoprotein (ABCB1) in Human and Rat Brain

2006 • 204 citations

Inhibition of the Multidrug Transporter P‐Glycoprotein Improves Seizure Control in Phenytoin‐treated Chronic Epileptic Rats

2006 • 204 citations

P-glycoprotein and multidrug resistance-associated protein are involved in the regulation of extracellular levels of the major antiepileptic drug carbamazepine in the brain

2001 • 201 citations

Cyclosporine markedly raises the plasma concentrations of repaglinide

2005 • 201 citations

Small molecular drug transfer across the blood-brain barrier via carrier-mediated transport systems

2004 • 200 citations

Expression and functional characterization of ABCG2 in brain endothelial cells and vessels

2003 • 200 citations

Occludin as direct target for glucocorticoid‐induced improvement of blood–brain barrier properties in a murinein vitrosystem

2005 • 200 citations

ABC Transporter (P-gp/ABCB1, MRP1/ABCC1, BCRP/ABCG2) Expression in the Developing Human CNS

2008 • 197 citations

Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.

2001 • 195 citations

Expression and Cellular Distribution of Multidrug Resistance–related Proteins in the Hippocampus of Patients with Mesial Temporal Lobe Epilepsy

2004 • 195 citations

A randomized, double-blind, placebo-controlled, phase 2 study of RMP-7 in combination with carboplatin administered intravenously for the treatment of recurrent malignant glioma

2003 • 190 citations

In Vivo Activation of Human Pregnane X Receptor Tightens the Blood-Brain Barrier to Methadone through P-Glycoprotein Up-Regulation

2006 • 187 citations

Expression and transcriptional regulation of ABC transporters and cytochromes P450 in hCMEC/D3 human cerebral microvascular endothelial cells

2008 • 187 citations

Expression of Drug Resistance Proteins Pgp, MRP1, MRP3, MRP5 AND GST-π in Human Glioma

2005 • 187 citations

Application of Three-Dimensional Quantitative Structure-Activity Relationships of P-Glycoprotein Inhibitors and Substrates

2002 • 186 citations

In Vivo Evidence for P‐Glycoprotein–Mediated Transport of Phenytoin at the Blood–Brain Barrier of Rats

2001 • 185 citations

Effects of adrenal cortical steroids and osmotic blood-brain barrier opening on methotrexate delivery to gliomas in the rodent: the factor of the blood-brain barrier.

1982 • 184 citations

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

1998 • 182 citations

Overview of the Proton-coupled MCT (SLC16A) Family of Transporters: Characterization, Function and Role in the Transport of the Drug of Abuse γ-Hydroxybutyric Acid

2008 • 182 citations

Interaction of Methotrexate with Organic-Anion Transporting Polypeptide 1A2 and Its Genetic Variants

2006 • 181 citations

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

1999 • 180 citations

Use of Verapamil as a Potential P-Glycoprotein Inhibitor in a Patient with Refractory Epilepsy

2004 • 177 citations

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

1994 • 174 citations

Plasma Membrane Localization of Multidrug Resistance-Associated Protein Homologs in Brain Capillary Endothelial Cells

2004 • 174 citations

Effect of age on functional P-glycoprotein in the blood-brain barrier measured by use of (R)-[11C]verapamil and positron emission tomography

2006 • 174 citations

Modulation of the blood–brain barrier in oncology: therapeutic opportunities for the treatment of brain tumours?

2004 • 173 citations

P-Glycoprotein Limits Oral Availability, Brain, and Fetal Penetration of Saquinavir Even with High Doses of Ritonavir

2001 • 171 citations

Progress in Brain Penetration Evaluation in Drug Discovery and Development

2008 • 168 citations

Recent Advances in Blood–Brain Barrier Disruption as a CNS Delivery Strategy

2008 • 168 citations

S -Ketamine Anesthesia Increases Cerebral Blood Flow in Excess of the Metabolic Needs in Humans

2005 • 162 citations

Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat.

1999 • 162 citations

Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3

2008 • 162 citations

Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans

2004 • 161 citations

A review on the impact of P-glycoprotein on the penetration of drugs into the brain. Focus on psychotropic drugs

2007 • 159 citations

Potential role of ABC transporters as a detoxification system at the blood?CSF barrier

2004 • 157 citations

Comparison of Brain Extracellular Fluid, Brain Tissue, Cerebrospinal Fluid, and Serum Concentrations of Antiepileptic Drugs Measured Intraoperatively in Patients with Intractable Epilepsy

2006 • 155 citations

Functional relevance of carnitine transporter OCTN2 to brain distribution of<scp>l</scp>‐carnitine and acetyl‐<scp>l</scp>‐carnitine across the blood–brain barrier

2001 • 155 citations

Role of P-glycoprotein in the intestinal absorption and clinical effects of morphine

2003 • 154 citations

Ventricular Choline Transport

2001 • 154 citations

Dose Escalation Studies of Cytarabine, Daunorubicin, and Etoposide With and Without Multidrug Resistance Modulation With PSC-833 in Untreated Adults With Acute Myeloid Leukemia Younger Than 60 Years: Final Induction Results of Cancer and Leukemia Group B Study 9621

2004 • 153 citations

Characterization of two splice variants of human organic anion transporting polypeptide 3A1 isolated from human brain

2006 • 153 citations

Treatment of Refractory and Relapsed Acute Myelogenous Leukemia With Combination Chemotherapy Plus the Multidrug Resistance Modulator PSC 833 (Valspodar)

1999 • 152 citations

Calcium‐channel Blocker Verapamil Administration in Prolonged and Refractory Status Epilepticus

2005 • 147 citations

Synthetic and natural opiates interact with P-glycoprotein in multidrug-resistant cells

1993 • 142 citations

Cerebrospinal fluid pharmacokinetics and penetration of continuous infusion topotecan in children with central nervous system tumors

1995 • 141 citations

Differential expression of the multidrug resistance‐related proteins ABCb1 and ABCc1 between blood‐brain interfaces

2008 • 140 citations

Quantitative Investigation of the Role of Breast Cancer Resistance Protein (Bcrp/Abcg2) in Limiting Brain and Testis Penetration of Xenobiotic Compounds

2008 • 140 citations

Dexamethasone increases expression and activity of multidrug resistance transporters at the rat blood-brain barrier

2008 • 139 citations

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

2008 • 137 citations

A new in vivo method to study P-glycoprotein transport in tumors and the blood-brain barrier.

1999 • 135 citations

Distinct spatio‐temporal expression of ABCA and ABCG transporters in the developing and adult mouse brain

2005 • 132 citations

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

2005 • 123 citations

Xenobiotic Transporters: Ascribing Function from Gene Knockout and Mutation Studies

2007 • 122 citations

Distinct regional distribution of human equilibrative nucleoside transporter proteins 1 and 2 (hENT1 and hENT2) in the central nervous system

2001 • 121 citations

Expression of Multidrug Transporters MRP1, MRP2, and BCRP Shortly after Status Epilepticus, during the Latent Period, and in Chronic Epileptic Rats

2005 • 120 citations

Investigation of Efflux Transport of Dehydroepiandrosterone Sulfate and Mitoxantrone at the Mouse Blood-Brain Barrier: A Minor Role of Breast Cancer Resistance Protein

2004 • 119 citations

Coordinated Nuclear Receptor Regulation of the Efflux Transporter, Mrp2, and the Phase-Ii Metabolizing Enzyme, GSTπ, at the Blood—Brain Barrier

2008 • 117 citations

Improved penetration of docetaxel into the brain by co-administration of inhibitors of P-glycoprotein

2004 • 116 citations

Phase II trial of intravenous lobradimil and carboplatin in childhood brain tumors: a report from the Children’s Oncology Group

2006 • 113 citations

Altered disposition of pravastatin following concomitant drug therapy with cyclosporin A in transplant recipients.

1993 • 113 citations

Up‐regulation of P‐glycoprotein by HIV protease inhibitors in a human brain microvessel endothelial cell line

2008 • 110 citations

Blood–Brain Barrier Transport of Valproic Acid

1985 • 108 citations

¹⁸F‐dopa PET evidence that tolcapone acts as a central COMT inhibitor in Parkinson's disease

2001 • 107 citations

Evaluation of Drug-Transporter Interactions Using In Vitro and In Vivo Models

2007 • 107 citations

Effects of ABCB1 (multidrug resistance transporter) gene mutations on disposition and central nervous effects of loperamide in healthy volunteers

2003 • 104 citations

Distributional transport kinetics of zidovudine between plasma and brain extracellular fluid/cerebrospinal fluid in the rabbit: investigation of the inhibitory effect of probenecid utilizing microdialysis.

1993 • 104 citations

Transport mechanism of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors at the blood-brain barrier.

1993 • 103 citations

Distribution and Expression of Soluble Epoxide Hydrolase in Human Brain

2008 • 102 citations

Methods to assess drug permeability across the blood-brain barrier

2006 • 102 citations

Tariquidar-Induced P-Glycoprotein Inhibition at the Rat Blood–Brain Barrier Studied with (R)-¹¹C-Verapamil and PET

2008 • 102 citations

Substrate Overlap between Mrp4 and Abcg2/Bcrp Affects Purine Analogue Drug Cytotoxicity and Tissue Distribution

2007 • 100 citations

Expression of Human Organic Anion Transporters in the Choroid Plexus and Their Interactions With Neurotransmitter Metabolites

2003 • 99 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

Increased toxicity of P-glycoprotein-substrate chemotherapeutic agents in a dog with the MDR1 deletion mutation associated with ivermectin sensitivity

2003 • 95 citations

Regulation of Drug and Bile Salt Transporters in Liver and Intestine

2003 • 93 citations

Mediation of Highly Concentrative Uptake of Pregabalin by L-Type Amino Acid Transport in Chinese Hamster Ovary and Caco-2 Cells

2005 • 92 citations

P-glycoprotein-mediated efflux of antiepileptic drugs: preliminary studies in mdr1a knockout mice

2002 • 92 citations

Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice

2007 • 92 citations

Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides.

2001 • 91 citations

Enhanced penetration of indinavir in cerebrospinal fluid and semen after the addition of low-dose ritonavir

2000 • 91 citations

The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice

2003 • 91 citations

Verapamil P-glycoprotein Transport across the Rat Blood-Brain Barrier: Cyclosporine, a Concentration Inhibition Analysis, and Comparison with Human Data

2006 • 90 citations

Effect of Osmotic Blood-Brain Barrier Disruption on Methotrexate Pharmacokinetics in the Dog

1980 • 90 citations

Organic anion transporter 3 is involved in the brain‐to‐blood efflux transport of thiopurine nucleobase analogs

2004 • 89 citations

Glucocorticoid effects on mouse microvascular endothelial barrier permeability are brain specific

2006 • 89 citations

Factors affecting delivery of antiviral drugs to the brain

2004 • 88 citations

The effects of salicylate and probenecid on the cerebrospinal fluid transport of penicillin, aminosalicyclic acid and iodide.

1974 • 88 citations

Morphine blood-brain barrier transport is influenced by probenecid co-administration.

2003 • 87 citations

P-glycoprotein-Mediated Active Efflux of the Anti-HIV1 Nucleoside Abacavir Limits Cellular Accumulation and Brain Distribution

2007 • 86 citations

Evaluation of in vivo P-glycoprotein function at the blood-brain barrier among MDR1 gene polymorphisms by using 11C-verapamil.

2006 • 86 citations

Quantitative in Vivo Microdialysis Study on the Influence of Multidrug Transporters on the Blood-Brain Barrier Passage of Oxcarbazepine: Concomitant Use of Hippocampal Monoamines as Pharmacodynamic Markers for the Anticonvulsant Activity

2005 • 86 citations

In Vivo Evaluation of P-glycoprotein Function at the Blood-Brain Barrier in Nonhuman Primates Using [¹¹C]Verapamil

2005 • 85 citations

Topotecan Central Nervous System Penetration Is Altered by a Tyrosine Kinase Inhibitor

2006 • 85 citations

Effect of ketoconazole on ritonavir and saquinavir concentrations in plasma and cerebrospinal fluid from patients infected with human immunodeficiency virus

2000 • 84 citations

¹¹C-Loperamide and Its N-Desmethyl Radiometabolite Are Avid Substrates for Brain Permeability-Glycoprotein Efflux

2008 • 83 citations

Quantitative assessment of P-glycoprotein function in the rat blood–brain barrier by distribution volume of [11C]verapamil measured with PET

2003 • 81 citations

Utility of Mdr1-Gene Deficient Mice in Assessing the Impact of P-glycoprotein on Pharmacokinetics and Pharmacodynamics in Drug Discovery and Development

2003 • 81 citations

Multidrug Resistance Protein 4 Protects Bone Marrow, Thymus, Spleen, and Intestine from Nucleotide Analogue–Induced Damage

2007 • 80 citations

Differential in Vivo Sensitivity to Inhibition of P-glycoprotein Located in Lymphocytes, Testes, and the Blood-Brain Barrier

2006 • 80 citations

Screening of multidrug-resistance sensitive drugs by in situ brain perfusion in P-glycoprotein-deficient mice.

2001 • 79 citations

RLIP76, a non-ABC transporter, and drug resistance in epilepsy

2005 • 78 citations

Assessment of the First and Second Generation Antihistamines Brain Penetration and Role of P-Glycoprotein

2006 • 78 citations

Biodistribution, radiation dose estimates, and in vivo Pgp modulation studies of 18F-paclitaxel in nonhuman primates.

2003 • 78 citations

Strategies for Increasing Drug Delivery to the Brain

2002 • 76 citations

Minocycline and riluzole brain disposition: interactions with p‐glycoprotein at the blood–brain barrier

2007 • 76 citations

Loperamide Toxicity in a Collie with the MDR1 Mutation Associated with Ivermectin Sensitivity

2004 • 75 citations

Disulfiram Metabolites Permanently Inactivate the Human Multidrug Resistance P-Glycoprotein

2004 • 75 citations

Quantitative evaluation of brain distribution and blood-brain barrier efflux transport of probenecid in rats by microdialysis: possible involvement of the monocarboxylic acid transport system.

1997 • 75 citations

The influence of C3435T polymorphism of ABCB1 gene on penetration of phenobarbital across the blood–brain barrier in patients with generalized epilepsy

2008 • 75 citations

TOTAL INTRAVENOUS ANESTHESIA

2007 • 75 citations

Acetyl‐<scp>L</scp>‐carnitine permeability across the blood–brain barrier and involvement of carnitine transporter OCTN2

2003 • 74 citations

Cellular localization of P-glycoprotein in brain versus gonadal capillaries.

1996 • 73 citations

In vitro and in vivo transport of zidovudine (AZT) across the blood-brain barrier and the effect of transport inhibitors.

1994 • 73 citations

Effect of P-glycoprotein inhibition on methadone analgesia and brain distribution in the rat

2004 • 73 citations

Uptake of valproic acid into rat brain is mediated by a medium-chain fatty acid transporter.

1996 • 72 citations

Investigation of the Role of Breast Cancer Resistance Protein (Bcrp/Abcg2) on Pharmacokinetics and Central Nervous System Penetration of Abacavir and Zidovudine in the Mouse

2008 • 71 citations

Pharmacokinetic Considerations in the Treatment of CNS Tumours

2006 • 71 citations

GHB (γ-Hydroxybutyrate) Carrier-Mediated Transport across the Blood-Brain Barrier

2004 • 70 citations

Modulation of P-glycoprotein Transport Activity in the Mouse Blood-Brain Barrier by Rifampin

2003 • 70 citations

Influence of functional haplotypes in the drug transporter gene on central nervous system drug distribution in humans

2005 • 68 citations

Methods to Assess Tissue-Specific Distribution and Metabolism of Drugs

2004 • 68 citations

Cerebral uptake of mefloquine enantiomers with and without the P‐gp inhibitor elacridar (GF1210918) in mice

2004 • 68 citations

Modulation of the Brain Distribution of Imatinib and its Metabolites in Mice by Valspodar, Zosuquidar and Elacridar

2007 • 67 citations

P-Glycoprotein Function at the Blood–Brain Barrier Imaged Using ¹¹C-N-Desmethyl-Loperamide in Monkeys

2008 • 66 citations

Species Differences of Inhibitory Effects on P‐glycoprotein‐mediateD Drug Transport

2006 • 66 citations

Apparent lack of Mrp1-mediated efflux at the luminal side of mouse blood-brain barrier endothelial cells.

2003 • 66 citations

In Vitro-to-in Vivo Prediction of P-glycoprotein-Based Drug Interactions at the Human and Rodent Blood-Brain Barrier

2007 • 64 citations

Increased CNS uptake and enhanced antinociception of morphine‐6‐glucuronide in rats after inhibition of P‐glycoprotein

2002 • 64 citations

Randomized Study of Paclitaxel and Tamoxifen Deposition into Human Brain Tumors: Implications for the Treatment of Metastatic Brain Tumors

2006 • 64 citations

Antidote Use in the Critically Ill Poisoned Patient

2006 • 61 citations

Choroid plexus epithelial monolayers – a cell culture model from porcine brain

2006 • 60 citations

Dose-dependent brain penetration of SDZ PSC 833, a novel multidrug resistance-reversing cyclosporin, in rats

1996 • 60 citations

Pharmacokinetics of methotrexate in cerebrospinal fluid and serum after osmotic blood-brain barrier disruption in patients with brain lymphoma

2000 • 60 citations

Inhibition of P-glycoprotein Activity at the Primate Blood-Brain Barrier Increases the Distribution of Nelfinavir into the Brain but Not into the Cerebrospinal Fluid

2007 • 59 citations

The distribution of the anti‐HIV drug, 2′3′‐dideoxycytidine (ddC), across the blood–brain and blood–cerebrospinal fluid barriers and the influence of organic anion transport inhibitors

2002 • 59 citations

MONOAMINE OXIDASES OF THE HUMAN BRAIN AND LIVER

1988 • 59 citations

Glucocorticoids Increase VE-Cadherin Expression and Cause Cytoskeletal Rearrangements in Murine Brain Endothelial cEND Cells

2008 • 58 citations

Localization of organic cation/carnitine transporter (OCTN2) in cells forming the blood–brain barrier

2007 • 58 citations

Effect of 21-day exposure of phenobarbital, carbamazepine and phenytoin on P-glycoprotein expression and activity in the rat brain

2008 • 57 citations

Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine

1997 • 57 citations

Duration and degree of cyclosporin induced P-glycoprotein inhibition in the rat blood–brain barrier can be studied with PET

2006 • 56 citations

Interaction of Ritonavir-Boosted Tipranavir with Loperamide Does Not Result in Loperamide-Associated Neurologic Side Effects in Healthy Volunteers

2005 • 56 citations

The role of membrane transporters in drug delivery to brain tumors

2007 • 56 citations

Induction of Nuclear Receptors and Drug Resistance in the Brain Microvascular Endothelial Cells Treated with Antiepileptic Drugs

2008 • 55 citations

Disulfiram Inhibits Defluorination of 18F-FCWAY, Reduces Bone Radioactivity, and Enhances Visualization of Radioligand Binding to Serotonin 5-HT1A Receptors in Human Brain

2007 • 54 citations

CEREBRAL UPTAKE OF DRUGS IN HUMANS

2007 • 54 citations

No effect of MDR1 C3435T variant on loperamide disposition and central nervous system effects

2003 • 54 citations

Brain Protection at the Blood–Cerebrospinal Fluid Interface Involves a Glutathione-Dependent Metabolic Barrier Mechanism

2006 • 54 citations

The effect of vigabatrin (γ-vinyl GABA) on cerebral blood flow and metabolism

1999 • 53 citations

Acidic drug transport in vivo through the blood-brain barrier. A role of the transport carrier for monocarboxylic acids.

1990 • 53 citations

Pharmacokinetics of lamivudine and BCH-189 in plasma and cerebrospinal fluid of nonhuman primates

1995 • 52 citations

Involvement of the Multidrug Resistance Protein 3 in Drug Sensitivity and Its Expression in Human Glioma

2001 • 52 citations

Pharmacokinetics of 3'-azido-3'-deoxythymidine and its catabolites and interactions with probenecid in rhesus monkeys

1991 • 52 citations

Cyclophosphamide and ifosfamide metabolites in the cerebrospinal fluid of children.

1997 • 52 citations

Brain distribution of 6-mercaptopurine is regulated by the efflux transport system in the blood-brain barrier 1

2000 • 52 citations

Multidrug resistance-reversing agents increase vinblastine distribution in normal tissues expressing the P-glycoprotein but do not enhance drug penetration in brain and testis.

1997 • 52 citations

Localization of organic anion transporting polypeptide 3 (oatp3) in mouse brain parenchymal and capillary endothelial cells

2004 • 52 citations

Microdialysis studies of the distribution of stavudine into the central nervous system in the freely-moving rat.

1997 • 51 citations

Ritonavir increases loperamide plasma concentrations without evidence for P‐glycoprotein involvement

2001 • 51 citations

P-glycoprotein interaction with risperidone and 9-OH-risperidone studiedin vitro, in knock-out mice and in drug-drug interaction experiments

2005 • 51 citations

Detection of benzodiazepine receptor occupancy in the human brain by positron emission tomography

1989 • 50 citations

Effect of plasma levels of large neutral amino acids and degree of parkinsonism on the blood‐to‐brain transport of levodopa in naive and MPTP parkinsonian monkeys

1994 • 48 citations

Central analgesic actions of loperamide following transient permeation of the blood brain barrier with Cereport™ (RMP-7)

1998 • 48 citations

Expression of nuclear receptor mRNA and liver X receptor-mediated regulation of ABC transporter A1 at rat blood–brain barrier

2007 • 47 citations

New positron emission tomography tracer [¹¹C]carvedilol reveals P‐glycoprotein modulation kinetics

2005 • 47 citations

Simultaneous PET Imaging of P-Glycoprotein Inhibition in Multiple Tissues in the Pregnant Nonhuman Primate

2009 • 47 citations

Decreased Phenytoin Level During Antineoplastic Therapy: A Case Report

1983 • 45 citations

Population pharmacokinetic analysis of drug–drug interactions among risperidone, bupropion, and sertraline in CF1 mice

2005 • 45 citations

P-Glycoprotein Contributes to the Blood-Brain, but Not Blood-Cerebrospinal Fluid, Barrier in a Spontaneous Canine P-Glycoprotein Knockout Model

2008 • 45 citations

Active transport of methotrexate from cerebrospinal fluid in humans.

1980 • 44 citations

Imaging treatment effects in Alzheimer's disease

2007 • 44 citations

Effects of Ritonavir on Indinavir Pharmacokinetics in Cerebrospinal Fluid and Plasma

2003 • 41 citations

The Distribution of the HIV Protease Inhibitor, Ritonavir, to the Brain, Cerebrospinal Fluid, and Choroid Plexuses of the Guinea Pig

2003 • 41 citations

Association of ABCB1 genetic variants 3435C&gt;T and 2677G&gt;T to ABCB1 mRNA and protein expression in brain tissue from refractory epilepsy patients

2008 • 41 citations

The effect of dexamethasone on the uptake of cisplatin in 9L glioma and the area of brain around tumor.

1998 • 40 citations

Relationship Between Drugs and Functional Activity of Various Mammalian P-Glycoproteins (ABCB1)

2008 • 40 citations

Loperamide poisoning in the dog.

1996 • 40 citations

Dexamethasone and Enhancing Solitary Cerebral Mass Lesions: Alterations in Perfusion and Blood-tumor Barrier Kinetics Shown by Magnetic Resonance Imaging

2006 • 39 citations

Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement

2001 • 39 citations

Glucocorticoids regulate the human occludin gene through a single imperfect palindromic glucocorticoid response element

2008 • 38 citations

Effect of antihypertensive agents on cerebral blood flow and flow velocity in acute ischaemic stroke: systematic review of controlled studies

2008 • 38 citations

Differential permeability of a human brain tumor xenograft in the nude rat: impact of tumor size and method of administration on optimizing delivery of biologically diverse agents.

1998 • 38 citations

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

2000 • 36 citations

Localization of P-glycoprotein at the nuclear envelope of rat brain cells

2007 • 34 citations

The Impact of Pharmacologic and Genetic Knockout of P-Glycoprotein on Nelfinavir Levels in the Brain and Other Tissues in Mice

2005 • 34 citations

Mechanisms by which 2′,3′‐dideoxyinosine (ddI) crosses the guinea‐pig CNS barriers; relevance to HIV therapy

2003 • 33 citations

Dynamics of multidrug resistance: P-glycoprotein analyses with positron emission tomography

2002 • 33 citations

Organic Anion‐Transporting Polypeptides at the Blood–Brain and Blood–Cerebrospinal Fluid Barriers

2007 • 33 citations

Favourable effects of nilvadipine on cognitive function and regional cerebral blood flow on SPECT in hypertensive patients with mild cognitive impairment

2007 • 33 citations

Scaling of in Vitro Membrane Permeability to Predict P-glycoprotein-Mediated Drug Absorption in Vivo

2008 • 32 citations

Zidovudine Transport within the Rabbit Brain during Intracerebroventricular Administration and the Effect of Probenecid

1997 • 32 citations

Transport of valproate at intestinal epithelial (Caco-2) and brain endothelial (RBE4) cells: Mechanism and substrate specificity

2008 • 31 citations

Tariquidar, a Selective P-glycoprotein Inhibitor, Does Not Potentiate Loperamide’s Opioid Brain Effects in Humans despite Full Inhibition of Lymphocyte P-glycoprotein

2008 • 31 citations

β-Adrenergic regulation of amine precursor amino acid transport across the blood-brain barrier

1992 • 31 citations

Barrier mechanisms for neurotransmitter monoamines in the choroid plexus

1980 • 31 citations

Differential permeability and quantitative MR imaging of a human lung carcinoma brain xenograft in the nude rat.

1995 • 30 citations

Hydroxyurea transport across the blood–brain and blood–cerebrospinal fluid barriers of the guinea‐pig

2003 • 28 citations

Enhancing the uptake of dextromethorphan in the CNS of rats by concomitant administration of the P-gp inhibitor verapamil

2005 • 28 citations

Levodopa effect on [18F]fluorodopa influx to brain: normal volunteers and patients with Parkinson's disease

2004 • 28 citations

The accumulation of topotecan in 9L glioma and in brain parenchyma with and without dexamethasone administration.

1999 • 26 citations

Cyclosporin A inhibits the extrusion pump function of p-glycoprotein in the inner ear of mice treated with vinblastine and doxorubicin

2001 • 26 citations

Lack of Support for a Role for RLIP76 (RALBP1) in Response to Treatment or Predisposition to Epilepsy

2007 • 26 citations

Potentiation of domperidone‐induced catalepsy by a P‐glycoprotein inhibitor, cyclosporin A

2003 • 26 citations

Facilitated transport of cefodizime into the rat central nervous system.

1991 • 24 citations

DEPENDENCE OF NELFINAVIR BRAIN UPTAKE ON DOSE AND TISSUE CONCENTRATIONS OF THE SELECTIVE P-GLYCOPROTEIN INHIBITOR ZOSUQUIDAR IN RATS

2006 • 23 citations

The Origin of Deoxynucleosides in Brain: Implications for the Study of Neurogenesis and Stem Cell Therapy

2007 • 23 citations

Probenecid Interacts with the Pharmacokinetics of Morphine-6-glucuronide in Humans

2004 • 23 citations

Efflux of zidovudine and 2',3'-dideoxyinosine out of the cerebrospinal fluid when administered alone and in combination to Macaca nemestrina.

1994 • 21 citations

Tamoxifen Paradoxically Decreases Paclitaxel Deposition into Cerebrospinal Fluid of Brain Tumor Patients

2006 • 21 citations

Effect of Transport Inhibitors and Additional Anti-HIV Drugs on the Movement of Lamivudine (3TC) across the Guinea Pig Brain Barriers

2003 • 20 citations

Tetraparesis associated with colchicine is probably due to inhibition by verapamil of the P-glycoprotein efflux pump in the blood-brain barrier

2005 • 20 citations

Can celecoxib affect P-glycoprotein-mediated drug efflux? A microPET study

2008 • 19 citations

Nevirapine Uptake into the Central Nervous System of the Guinea Pig: An in Situ Brain Perfusion Study

2006 • 19 citations

Isoprenaline increases brain concentrations of administered l-dopa and l-tryptophan in the rat

1982 • 19 citations

Loperamide Toxicity in a Collie with the MDR1 Mutation Associated with Ivermectin Sensitivity

2004 • 18 citations

Effect of probenecid on cerebrospinal fluid methotrexate kinetics

1979 • 16 citations

Involvement of Rat Organic Anion Transporter 3 in the Uptake of an Organic Herbicide, 2,4-Dichlorophenoxyacetate, by the isOlated Rat Choroid Plexus

2004 • 16 citations

Transport of the beta-lactam antibiotic benzylpenicillin and the dipeptide glycylsarcosine by brain capillary endothelial cells in vitro.

1998 • 15 citations

Effect of lamotrigine on cerebral blood flow in patients with idiopathic generalised epilepsy

2006 • 15 citations

β‐Adrenergics enhance brain extraction of levodopa

2002 • 13 citations

Inhibition of methotrexate transport from cerebrospinal fluid by probenecid.

1976 • 12 citations

Potential γ-Hydroxybutyric acid (GHB) Drug Interactions Through Blood–Brain Barrier Transport Inhibition: A Pharmacokinetic Simulation-Based Evaluation

2006 • 11 citations

Drug transfer into cerebrospinal fluid after simultaneous administration of ampicillin with ceftriaxone or ceftazidime in rabbits with Staphylococcus aureus meningitis

1988 • 8 citations

Effect of probenecid on ventricular cerebrospinal fluid methotrexate pharmacokinetics after intralumbar administration in nonhuman primates

2001 • 8 citations

Vincristine effect on methotrexate cerebrospinal fluid concentration.

1979 • 8 citations

Probenecid inhibition of methotrexate-cerebrospinal fluid pharmacokinetics in dogs.

1978 • 8 citations

Methotrexate-vindesine association in leukemia: Pharmacokinetic study

1985 • 5 citations

The Effect of Amitriptyline on the Central Nervous System Penetration of Methotrexate

1986 • 3 citations

Deleted Work

1955 • 0 citations