Species Comparison of In Vivo P-Glycoprotein-Mediated Brain Efflux Using mdr1a-Deficient Rats and Mice

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Drug Metabolism And Disposition

• Publication date

  2012-03-01

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1124/dmd.111.043083PMID 22112383
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Characterization of Multidrug Resistance 1a/P-Glycoprotein Knockout Rats Generated by Zinc Finger Nucleases

  2012cited by this paper
• Strategies to optimize the brain availability of central nervous system drug candidates

  2011influential reference
• Induction of drug efflux protein expression by venlafaxine but not desvenlafaxine

  2011cited by this paper
• Effects on enantiomeric drug disposition and open-field behavior after chronic treatment with venlafaxine in the P-glycoprotein knockout mice model

  2011cited by this paper
• Measurement of Unbound Drug Exposure in Brain: Modeling of pH Partitioning Explains Diverging Results between the Brain Slice and Brain Homogenate Methods

  2011cited by this paper
• Structure−Activity Relationship Study of First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)

  2010cited by this paper
• Pharmacokinetics of acute and sub-chronic aripiprazole in P-glycoprotein deficient mice.

  2010influential reference
• Chronic stress and antidepressant treatment have opposite effects on P-glycoprotein at the blood—brain barrier: an experimental PET study in rats

  2010cited by this paper
• Comparative gene expression profiles of ABC transporters in brain microvessel endothelial cells and brain in five species including human.

  2009cited by this paper
• Knockout Rats via Embryo Microinjection of Zinc-Finger Nucleases

  2009cited by this paper
• Species Differences in Blood-Brain Barrier Transport of Three Positron Emission Tomography Radioligands with Emphasis on P-Glycoprotein Transport

  2009cited by this paper
• Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression.

  2008cited by this paper
• Relationship between drugs and functional activity of various mammalian P-glycoproteins (ABCB1).

  2008cited by this paper
• A review on the impact of P-glycoprotein on the penetration of drugs into the brain. Focus on psychotropic drugs.

  2008cited by this paper
• A REVIEW ON THE RELATION BETWEEN THE BRAIN-SERUM CONCENTRATION RATIO OF DRUGS AND THE INFLUENCE OF P-GLYCOPROTEIN

  2007cited by this paper
• Venlafaxine induces P‐glycoprotein in human Caco‐2 cells

  2007cited by this paper
• On The Rate and Extent of Drug Delivery to the Brain

  2007cited by this paper
• Establishment and Characterization of the Transformants Stably-Expressing MDR1 Derived from Various Animal Species in LLC-PK1

  2006cited by this paper
• BRAIN DISTRIBUTION OF CETIRIZINE ENANTIOMERS: COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS: Kp, Kp,u, AND Kp,uu

  2006cited by this paper
• Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier.

  2006cited by this paper
• Ensembl 2007

  2006cited by this paper
• Development and characterization of LLC-PK1 cells containing Sprague-Dawley rat Abcb1a (Mdr1a): comparison of rat P-glycoprotein transport to human and mouse.

  2006cited by this paper
• Kinetic analyses for species differences in P-glycoprotein-mediated drug transport.

  2006cited by this paper
• OF CETIRIZINE ENANTIOMERS : COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS

  2006cited by this paper
• P‐glycoprotein interaction with risperidone and 9‐OH‐risperidone studied in vitro, in knock‐out mice and in drug–drug interaction experiments

  2005cited by this paper
• 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

  2005cited by this paper
• The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein.

  2004cited by this paper
• Expression, up-regulation, and transport activity of the multidrug-resistance protein Abcg2 at the mouse blood-brain barrier.

  2004cited by this paper
• abcb1ab P-glycoprotein is involved in the uptake of citalopram and trimipramine into the brain of mice.

  2003cited by this paper
• Differential expression of multidrug resistance genes in naïve rat brain.

  2003cited by this paper
• Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery

  2002cited by this paper
• Transport mechanisms for the antidepressant citalopram in brain microvessel endothelium.

  1999cited by this paper
• Drug Equilibration Across the Blood—Brain Barrier-Pharmacokinetic Considerations Based on the Microdialysis Method

  1997cited by this paper
• P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs.

  1996cited by this paper
• The three mouse multidrug resistance (mdr) genes are expressed in a tissue-specific manner in normal mouse tissues

  1989cited by this paper
• Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.

  1987cited by this paper

• Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly?

  2025influential citation
• ABC Family Gene Polymorphisms and Cognitive Functions Interact to Influence Antidepressant Efficacy

  2024cites this paper
• ABCB1 variants and sex affect serotonin transporter occupancy in the brain

  2022cites this paper
• Characterization of Aripiprazole Uptake Transporter in the Blood-Brain Barrier Model hCMEC/D3 Cells by Targeted siRNA Screening

  2022cites this paper
• Optimization of dose and route of administration of the P‐glycoprotein inhibitor, valspodar (PSC‐833) and the P‐glycoprotein and breast cancer resistance protein dual‐inhibitor, elacridar (GF120918) as dual infusion in rats

  2021cites this paper
• P-glycoprotein mediates the pharmacokinetic interaction of olanzapine with fluoxetine in rats.

  2021cites this paper
• Differences in P-glycoprotein activity in human and rodent blood–brain barrier assessed by mechanistic modelling

  2021cites this paper
• Intestinal Excretion, Intestinal Recirculation, and Renal Tubule Reabsorption Are Underappreciated Mechanisms That Drive the Distribution and Pharmacokinetic Behavior of Small Molecule Drugs.

  2021cites this paper
• Estimating efflux transporter-mediated disposition of molecules beyond the rule of five (bRo5) using transporter gene knockout rats.

  2020cites this paper
• Pharmacokinetic Modeling of the Impact of P-glycoprotein on Ondansetron Disposition in the Central Nervous System

  2020cites this paper
• A Practical Perspective on the Evaluation of Small Molecule CNS Penetration in Drug Discovery.

  2020cites this paper
• Formulation Strategies to Address Physiological and Anatomical Constraints for Improved Topical Ocular Drug Delivery

  2019cites this paper
• P-glycoprotein Restricts Ocular Penetration of Loperamide across the Blood-Ocular Barriers: a Comparative Study in Mdr1a Knock-out and Wild Type Sprague Dawley Rats

  2018cites this paper
• ABCB1 1199G>A Polymorphism Affects the Intracellular Accumulation of Antidepressants in LLC-PK1 Recombinant Cell Lines

  2018cites this paper
• Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances.

  2017cites this paper
• Possibility of Predicting Serotonin Transporter Occupancy From the In Vitro Inhibition Constant for Serotonin Transporter, the Clinically Relevant Plasma Concentration of Unbound Drugs, and Their Profiles for Substrates of Transporters.

  2017cites this paper
• Target-Site Investigation for the Plasma Prolactin Response: Mechanism-Based Pharmacokinetic-Pharmacodynamic Analysis of Risperidone and Paliperidone in the Rat

  2017cites this paper
• Examining the Uptake of Central Nervous System Drugs and Candidates across the Blood-Brain Barrier

  2016cites this paper
• Measuring citalopram in blood and central nervous system: revealing a distribution pattern that differs from other antidepressants

  2016cites this paper
• Investigation of imatinib loaded surface decorated biodegradable nanocarriers against glioblastoma cell lines: Intracellular uptake and cytotoxicity studies.

  2016cites this paper
• P-glycoprotein differentially affects escitalopram, levomilnacipran, vilazodone and vortioxetine transport at the mouse blood-brain barrier in vivo.

  2016cites this paper
• Association of ABCB1 gene variants, plasma antidepressant concentration, and treatment response: Results from a randomized clinical study.

  2016cites this paper
• Morphometric analysis of the cerebral expression of ATP-binding cassette transporter protein ABCB1 in chronic schizophrenia: Circumscribed deficits in the habenula.

  2016cites this paper
• ABCB1 genotyping in the treatment of depression.

  2016cites this paper
• Recognition Mechanism of Dibenzoylhydrazines by Human P-glycoprotein

  2016cites this paper
• Blood-Brain Barrier Methods

  2016cites this paper
• The Use of Genetically Modified Animals in Discovery Toxicology

  2016cites this paper
• In vitro and in vivo evaluations of the P-glycoprotein-mediated efflux of dibenzoylhydrazines.

  2016cites this paper
• Differential role of P-glycoprotein and breast cancer resistance protein in drug distribution into brain, CSF and peripheral nerve tissues in rats

  2015cites this paper
• ABCB1 gene variants and antidepressant treatment outcome: A meta‐analysis

  2015influential citation
• Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation.

  2015influential citation
• In Vivo Studies of Brain Exposure in Drug Discovery

  2015cites this paper
• Designing Peripheral Drugs for Minimal Brain Exposure

  2015cites this paper
• Drugs, genes and the blues: pharmacogenetics of the antidepressant response from mouse to man.

  2014cites this paper
• Use of Cassette Dosing Approach to Examine the Effects of P-Glycoprotein on the Brain and Cerebrospinal Fluid Concentrations in Wild-Type and P-Glycoprotein Knockout Rats

  2014cites this paper
• Brain Penetration of WEB 2086 (Apafant) and Dantrolene in Mdr1a (P-Glycoprotein) and Bcrp Knockout Rats

  2014cites this paper
• DMD058545 1761..1765

  2014cites this paper
• Coadministration of P-Glycoprotein Modulators on Loperamide Pharmacokinetics and Brain Distribution

  2014influential citation
• Drug Discovery Methods for Studying Brain Drug Delivery and Distribution

  2014cites this paper
• DMD055566 700..706

  2014influential citation
• Human P-glycoprotein differentially affects antidepressant drug transport: relevance to blood-brain barrier permeability.

  2013cites this paper
• Minor Compensatory Changes in SAGE Mdr1a (P-gp), Bcrp, and Mrp2 Knockout Rats Do Not Detract from Their Utility in the Study of Transporter-Mediated Pharmacokinetics

  2013cites this paper
• Overview of Experimental Models of the Blood‐Brain Barrier in CNS Drug Discovery

  2013cites this paper
• PK/PD assessment in CNS drug discovery: Prediction of CSF concentration in rodents for P-glycoprotein substrates and application to in vivo potency estimation.

  2013cites this paper
• Insight into tissue unbound concentration: utility in drug discovery and development.

  2013cites this paper
• P-glycoprotein Inhibition Increases the Brain Distribution and Antidepressant-Like Activity of Escitalopram in Rodents

  2013cites this paper
• Pharmacogenetics of Chronic Pain and Its Treatment

  2013cites this paper
• Investigating the Enteroenteric Recirculation of Apixaban, a Factor Xa Inhibitor: Administration of Activated Charcoal to Bile Duct-Cannulated Rats and Dogs Receiving an Intravenous Dose and Use of Drug Transporter Knockout Rats

  2013cites this paper
• Microsoft Word-72067223-file00

  2013influential citation
• Altered brain concentrations of citalopram and escitalopram in P-glycoprotein deficient mice after acute and chronic treatment.

  2013cites this paper
• Co-administration of P-glycoprotein modulators on loperamide pharmacokinetics and brain distribution

  2013cites this paper
• DMD050575 906..915

  2013cites this paper
• Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 Knockout Rats Using Loperamide, Paclitaxel, Sulfasalazine, and Carboxydichlorofluorescein Pharmacokinetics

  2012influential citation
• paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics

  2012cites this paper
• Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood–brain barrier

  2012cites this paper
• Quantification of cytochromes P450, ABC transporters and their main transcription factors in the brains of alcoholics, smokers and drug-free controls by QRT-PCR

  2012cites this paper
• Microdialysis Evaluation of Clozapine and N-Desmethylclozapine Pharmacokinetics in Rat Brain

  2012cites this paper