(Q37681555)

22 August 2017

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title

Assessing brain free fraction in early drug discovery (English)

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22 August 2017

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Kevin D Read

1

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22 August 2017

Simone Braggio

series ordinal

2

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22 August 2017

language of work or name

English

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publication date

1 March 2010

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Expert Opinion on Drug Metabolism & Toxicology

22 August 2017

published in

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22 August 2017

volume

6

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22 August 2017

issue

3

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22 August 2017

page(s)

337-344

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Strategies to assess blood-brain barrier penetration

22 August 2017

cites work

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

An overview of in vitro techniques for blood-brain barrier studies

21 January 2018

1 reference

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The role of blood-brain barrier studies in the pharmaceutical industry

21 January 2018

1 reference

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Comparison of blood-brain barrier permeability assays: in situ brain perfusion, MDR1-MDCKII and PAMPA-BBB.

21 January 2018

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https://api.crossref.org/works/10.1517%2F17425250903559873

Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction

21 January 2018

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https://api.crossref.org/works/10.1517%2F17425250903559873

On the rate and extent of drug delivery to the brain.

21 January 2018

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Methodologies to assess brain drug delivery in lead optimization

21 January 2018

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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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Considerations in the use of cerebrospinal fluid pharmacokinetics to predict brain target concentrations in the clinical setting: implications of the barriers between blood and brain.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery.

21 January 2018

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CSF as a surrogate for assessing CNS exposure: an industrial perspective

21 January 2018

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Evidence for bulk flow of brain interstitial fluid: significance for physiology and pathology

21 January 2018

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Evaluation of cerebrospinal fluid concentration and plasma free concentration as a surrogate measurement for brain free concentration.

21 January 2018

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Differential, strain-specific cellular and subcellular distribution of multidrug transporters in murine choroid plexus and blood-brain barrier.

21 January 2018

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

21 January 2018

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Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids

21 January 2018

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Blood binding and tissue uptake of drugs. Recent advances and perspectives

21 January 2018

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Receptor occupancy and brain free fraction

21 January 2018

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Unbound brain concentration determines receptor occupancy: a correlation of drug concentration and brain serotonin and dopamine reuptake transporter occupancy for eighteen compounds in rats.

21 January 2018

1 reference

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Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

The relationship between sodium channel inhibition and anticonvulsant activity in a model of generalised seizure in the rat.

21 January 2018

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Pharmacokinetics and pharmacodynamics of seven opioids in P-glycoprotein-competent mice: assessment of unbound brain EC50,u and correlation of in vitro, preclinical, and clinical data

21 January 2018

1 reference

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Blood-brain barrier transport helps to explain discrepancies in in vivo potency between oxycodone and morphine.

21 January 2018

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Predicting haloperidol occupancy of central dopamine D2 receptors from plasma levels.

21 January 2018

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Evaluation of the utility of brain slice methods to study brain penetration.

21 January 2018

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Development of a high-throughput brain slice method for studying drug distribution in the central nervous system

21 January 2018

1 reference

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Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: comparison of unbound concentration ratios to in vivo p-glycoprotein efflux ratios.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Toward an improved prediction of human in vivo brain penetration.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Challenges for blood-brain barrier (BBB) screening

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

Holy grails and in vitro blood–brain barrier models

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17425250903559873

10.1517/17425250903559873

21 January 2018

Identifiers

DOI

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22 August 2017

1 reference