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

A stereotaxic atlas of the rat brain

1967 • 4,710 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

Blood-Brain Barrier in Physiology and Medicine

1976 • 888 citations

The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates.

1994 • 850 citations

Congenital Jaundice in Rats with a Mutation in a Multidrug Resistance-Associated Protein Gene

1996 • 827 citations

The Concept of a Blood-Brain Barrier

1980 • 812 citations

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

1980 • 799 citations

Drug excretion mediated by a new prototype of polyspecific transporter

1994 • 637 citations

Overexpression of the gene encoding the multidrug resistance-associated protein results in increased ATP-dependent glutathione S-conjugate transport.

1994 • 621 citations

An in situ brain perfusion technique to study cerebrovascular transport in the rat

1984 • 538 citations

Physiology of the choroid plexus.

1971 • 495 citations

Mechanisms mediating renal secretion of organic anions and cations

1993 • 484 citations

Lower limits of cerebrovascular permeability to nonelectrolytes in the conscious rat

1978 • 444 citations

Kinetics of Neutral Amino Acid Transport Across the Blood‐Brain Barrier

1987 • 441 citations

ATP-dependent transport of glutathione S-conjugates by the multidrug resistance-associated protein.

1994 • 435 citations

Blood–Brain Barrier in Physiology and Medicine

1977 • 395 citations

Hepatobiliary secretion of organic compounds; molecular mechanisms of membrane transport

1995 • 385 citations

BLOOD-BRAIN BARRIER

1943 • 356 citations

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

1992 • 352 citations

Intrathecal chemotherapy: brain tissue profiles after ventriculocisternal perfusion.

1975 • 321 citations

Efflux of radiolabeled polyethylene glycols and albumin from rat brain

1981 • 311 citations

Peptide Drug Delivery to the Brain

1992 • 309 citations

Implications of the Blood-Brain Barrier and Its Manipulation

1989 • 308 citations

Thienamycin: development of imipenem-cilastatin

1983 • 305 citations

Active transport of Diodrast and phenolsulfonphthalein from cerebrospinal fluid to blood

1961 • 301 citations

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

1992 • 288 citations

Carbapenems, a new class of beta-lactam antibiotics

1985 • 283 citations

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

1995 • 265 citations

Drug entry into the brain

1979 • 235 citations

Expression of the MRP gene-encoded conjugate export pump in liver and its selective absence from the canalicular membrane in transport-deficient mutant hepatocytes.

1995 • 230 citations

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

1996 • 225 citations

Resistance modification by PSC-833, a novel non-immunosuppressive cyclosporin A

1991 • 218 citations

Recent advances in carrier-mediated hepatic uptake and biliary excretion of xenobiotics.

1996 • 218 citations

Methods for quantifying the transport of drugs across brain barrier systems

1981 • 214 citations

Potassium exchange between cerebrospinal fluid, plasma, and brain

1965 • 208 citations

Measurements of dog blood-brain transfer constants by ventriculocisternal perfusion

1975 • 207 citations

Cerebrovascular Permeability Coefficients to Sodium, Potassium, and Chloride

1986 • 198 citations

Functional expression and subcellular localization of an anion exchanger cloned from choroid plexus.

1990 • 186 citations

Phase I study of etoposide with SDZ PSC 833 as a modulator of multidrug resistance in patients with cancer.

1996 • 179 citations

Bovine Brain Microvessel Endothelial Cell Monolayers as a Model System for the Blood‐Brain Barriera

1987 • 177 citations

THE PASSAGE OF CERTAIN SUBSTANCES OUT OF THE CEREBROSPINAL FLUID

1963 • 177 citations

Specificity of transporters for ‘organic anions’ and ‘organic cations’ in the kidney

1994 • 172 citations

Blood-Brain and CSF Barriers to Penicillin and Related Organic Acids

1966 • 167 citations

Narcotics and the hypothalamus

1974 • 163 citations

The active transport of 5‐hydroxyindol‐3‐ylacetic acid and 3‐methoxy‐4‐hydroxyphenylacetic acid from a recirculatory perfusion system of the cerebral ventricles of the unanaesthetized dog

1968 • 162 citations

Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver.

1996 • 152 citations

Peptide transport systems for opiates across the blood-brain barrier

1990 • 140 citations

Drug “Diffusion” within the Brain^a

1988 • 134 citations

Central Nervous System Reactions to Histamine-2 Receptor Blockers

1991 • 133 citations

Central nervous system toxicity of quinolones: human and animal findings

1990 • 131 citations

Cerebrovascular permeability to peptides: manipulations of transport systems at the blood-brain barrier.

1995 • 128 citations

Quantitative studies of the passage of different substances out of the cerebro‐spinal fluid

1962 • 123 citations

Blood–Brain Barrier Transport of Valproic Acid

1985 • 108 citations

Blood-brain barrier function of P-glycoprotein

1997 • 108 citations

Distributed model for drug delivery to CSF and brain tissue

1983 • 105 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

Increase in the Content of Quinolinic Acid in Cerebrospinal Fluid and Frontal Cortex of Patients with Hepatic Failure

1986 • 91 citations

Micronutrient Homeostasis in Mammalian Brain and Cerebrospinal Fluid

1989 • 90 citations

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

1974 • 88 citations

Age, disease, and cimetidine disposition in healthy subjects and chronically ill patients

1981 • 86 citations

Identifying secondary active solute transport in epithelia

1981 • 86 citations

5-hydroxyindoleacetic acid accumulation by isolated choroid plexus

1971 • 86 citations

Bisubstrates: substances that interact with renal contraluminal organic anion and organic cation transport systems

1993 • 86 citations

The Anatomic Basis of the Blood-Brain Barrier

1989 • 83 citations

Inhibition of Penicillin Transport from the Cerebrospinal Fluid after Intracisternal Inoculation of Bacteria

1974 • 82 citations

A nonlinear least squares program, MULTI(FILT), based on fast inverse laplace transform for microcomputers.

1989 • 81 citations

Transport of material between brain extracellular fluid, brain cells and blood.

1974 • 80 citations

Study on brain interstitial fluid distribution and blood-brain barrier transport of baclofen in rats by microdialysis.

1995 • 80 citations

Active transport of quaternary ammonium compounds by the choroid plexus in vitro

1965 • 80 citations

Consensus report

1987 • 75 citations

The Concept of a Blood-Brain Barrier

1980 • 74 citations

Content of Quinolinic Acid and of Other Tryptophan Metabolites Increases in Brain Regions of Rats Used as Experimental Models of Hepatic Encephalopathy

1986 • 72 citations

Microdialysis study of zidovudine (AZT) transport in rat brain.

1993 • 70 citations

Bisubstrates: substances that interact with both, renal contraluminal organic anion and organic cation transport systems

1993 • 68 citations

Iodide and thiocyanate efflux from brain following injection into rat caudate nucleus

1978 • 60 citations

Vector-mediated peptide drug delivery to the brain

1995 • 55 citations

Evidence of active transport of benzyl-14C-penicillin from cerebrospinal fluid to blood

1969 • 54 citations

Sodium‐Dependent Antiporters in Choroid Plexus Epithelial Cultures from Rabbit

1993 • 54 citations

Transport of methotrexate by the choroid plexus.

1968 • 53 citations

Contribution of probenecid-sensitive anion transport processes at the brain capillary endothelium and choroid plexus to the efficient efflux of valproic acid from the central nervous system.

1994 • 53 citations

The effect of probenecid on the renal elimination of cimetidine

1989 • 51 citations

Influence of various drugs on the transport of ¹³¹I and PAH across the cerebrospinal‐fluid—blood barrier

1963 • 50 citations

Rapid efflux of some quaternary ammonium compounds from cerebrospinal fluid

1962 • 48 citations

Cimetidine secretion by rabbit renal tubules in vitro

1981 • 47 citations

Differential effects of acetazolamide, benzolamide and systemic acidosis on hydrogen and bicarbonate gradients across the apical and basolateral membranes of the choroid plexus.

1984 • 47 citations

The Choroid Plexus–Arachnoid Membrane–Cerebrospinal Fluid System

2003 • 46 citations

Interactions of organic anions with the organic cation transporter in renal BBMV

1988 • 46 citations

Active transport of 5-hydroxyindoleacetic acid by the rabbit choroid plexus in vitro

1972 • 45 citations

Kinetics of active efflux via choroid plexus of beta-lactam antibiotics from the CSF into the circulation

1994 • 45 citations

Transport of benzylpenicillin by the rat choroid plexus in vitro.

1987 • 44 citations

Transport across the Blood-Brain Barrier

1989 • 42 citations

Pharmacokinetics of intraventricular administration

1983 • 42 citations

Transport of cimetidine by the rat choroid plexus in vitro.

1986 • 42 citations

Ceftriaxone pharmacokinetics in the central nervous system.

1986 • 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

Saturable transport of cimetidine from cerebrospinal fluid to blood in rats.

1985 • 40 citations

Accumulation of anionic pesticides by rabbit choroid plexus in vitro.

1980 • 39 citations

Membrane potentials and sugar transport by ATP-depleted intestinal cells: effect of anion gradients

1979 • 39 citations

Potential for Pharmacologic Manipulation of the Blood-Cerebrospinal Fluid Barrier

1989 • 38 citations

Expression of a putative ATP-binding cassette region, homologous to that in multidrug resistance-associated protein (MRP), is hereditarily defective in Eisai hyperbilirubinemic rats (EHBR)

1996 • 38 citations

Transport of organic cations and anions by choroid plexus.

1976 • 38 citations

Ceftriaxone Transport Through the Blood-Brain Barrier

1987 • 37 citations

Anion exchanger mediates benzylpenicillin transport in rat choroid plexus.

1987 • 37 citations

Interaction of ofloxacin with organic cation transport system in rat renal brush-border membranes.

1990 • 36 citations

Cimetidine transport in isolated luminal membrane vesicles from rabbit kidney

1987 • 35 citations

Transport of imipenem, a novel carbapenem antibiotic, in the rat central nervous system.

1989 • 34 citations

Antibody delivery through the blood-brain barrier

1995 • 34 citations

History of the Blood-Brain Barrier Concept

1989 • 34 citations

Comparative distribution of quinolone antibiotics in cerebrospinal fluid and brain in rats and dogs.

1996 • 34 citations

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

1994 • 33 citations

On the active transport of organic acids (fluorescein) in the choroid plexus of the rabbit

1979 • 32 citations

Peptide Drug Delivery to the Brain

1992 • 32 citations

Renal handling of fleroxacin in rabbits, dogs, and humans

1990 • 30 citations

Antisense drug delivery through the blood-brain barrier

1995 • 29 citations

Transport of choline out of the cranial cerebrospinal fluid spaces of the rabbit.

1980 • 29 citations

Cimetidine transport in isolated brush border membrane vesicles from bovine choroid plexus.

1990 • 28 citations

Active transport of chloride by lateral ventricle choroid plexus of the rat

1985 • 28 citations

Riboflavin transport in the central nervous system. Characterization and effects of drugs.

1980 • 27 citations

Histamine H2-Antagonists-Past, Present and Future

1983 • 26 citations

Distribution of two model amino acids from cerebrospinal fluid to brain and blood

1982 • 26 citations

Cl-HCO3 exchange in choroid plexus: analysis by the DMO method for cell pH

1985 • 25 citations

Nucleoside and Vitamin Homeostasis in the Mammalian Central Nervous System

1986 • 25 citations

Renal secretion of organic cations: a multistep process

1997 • 24 citations

Facilitated transport of cefodizime into the rat central nervous system.

1991 • 24 citations

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

1989 • 22 citations

Purines: Active Transport by Isolated Choroid Plexus

1969 • 22 citations

Cimetidine transport in rabbit renal cortical brush-border membrane vesicles

1987 • 22 citations

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

1996 • 22 citations

Diffusion of penicillin in agar and cerebral cortex of the rat

1988 • 21 citations

Histamine H2-receptor antagonists and gastric acid secretion

1984 • 19 citations

FACILITATED TRANSPORT OF BENZYLPENICILLIN THROUGH THE BLOOD-BRAIN BARRIER IN RATS

1989 • 19 citations

Polysubstrates: substances that interact with renal contraluminal PAH, sulfate, and NMeN transport: sulfamoyl-, sulfonylurea-, thiazide- and benzeneamino-carboxylate (nicotinate) compounds.

1994 • 19 citations

A comparison of ampicillin-cefotaxime and ampicillin-chloramphenicol in childhood bacterial meningitis: an experience in 55 patients

1984 • 18 citations

Primary cell culture of the rabbit choroid plexus: an experimental system to investigate membrane transport.

1996 • 18 citations

Mechanisms of interactions between organic anions and the organic cation transporter in renal brush border membrane vesicles

1990 • 18 citations

Transport of DMO out of cerebrospinal fluid of rats

1970 • 17 citations

The active transport of para-aminosalicylic acid from the cerebrospinal fluid.

1973 • 17 citations

Transport of 2,4,5-trichlorophenoxyacetic acid across the blood-cerebrospinal fluid barrier of the rabbit.

1993 • 17 citations

Kinetic model for disposition of 6-mercaptopurine in monkey plasma and cerebrospinal fluid

1985 • 17 citations

Efflux of cimetidine from the rat cerebrospinal fluid.

1988 • 16 citations

The effect of uremia on penicillin flux between blood and cerebrospinal fluid.

1976 • 16 citations

Kinetics of quinolone antibiotics in rats: efflux from cerebrospinal fluid to the circulation.

1996 • 15 citations

Renal tubular secretion of organic anions

1997 • 15 citations

The partitioning of cimetidine into canine cerebrospinal fluid.

1984 • 13 citations

Genetically engineered antibodies and their application to brain delivery

1995 • 11 citations

Cefsulodin Penetration into Rat Brain: Extracellular versus Total Concentration

1986 • 10 citations

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

1988 • 8 citations

Comparative uptake of cimetidine by rat choroid plexus between the lateral and the 4th ventricles.

1986 • 7 citations

Cerebrospinal fluid penetration after combined administration of cefotaxime and ampicillin to rabbits with staphylococcal meningitis

1984 • 5 citations

Pharmacokinetics in the cerebrospinal fluid after simultaneous administration of latamoxef and ampicillin to rabbits with staphylococcal meningitis.

1984 • 5 citations

Effect of benzylpenicillin on the disposition of cefodizime in rats: no net effect on total clearance due to decreased hepatobiliary clearance and increased renal clearance.

1992 • 4 citations

Organic anion transport system acting as an efflux pump at the blood-brain barrier: Demonstration by a newly developed brain efflux index (BEI) method

1995 • 4 citations

[Transferability of biapenem (L-627) to cerebrospinal fluid in rabbits with meningitis caused by Staphylococcus aureus].

1994 • 3 citations

Cimetidine elimination from the cerebrospinal fluid of the rat.

1988 • 3 citations

Bile acid efflux transport system at the blood-brain barrier: Demonstration by the brain efflux index (BEI) method

1996 • 1 citations

[Experimental study on transferability to cerebrospinal fluid of cefodizime in combination with ampicillin].

1989 • 1 citations