The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity.

The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity. Research Abstract Details 

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The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity. Abstract Text:

Urban Fagerholm,Urban Fagerholm,

The blood-brain barrier is often perceived as relatively impermeable, and various cut-off values for zero or limited brain permeability have been suggested. The validity of these values has been evaluated in this review. The barrier appears to have a very high permeability and absorptive capacity: sufficient to absorb compounds with polar surface area >270 A(2), molecular weight > 1,000 Da, log D < -3.5 and equilibrium brain-to-blood concentration ratio <0.01 well. Sufficient intestinal uptake indicates good passive brain uptake potential. The uptake is potentially more sensitive to involvement and changes of active transport than in the intestines. A physiologically based in vitro-in vivo method for prediction of brain uptake is presented.

The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity. Publishing Authors By Initials

U Fagerholm,U Fagerholm,

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The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Drug discovery today

VOLUME: 12

Page Numbers: 1076-82

Journal Abbreviation: Drug Discov. Today

ISSN: 1359-6446

DAY: 26

MONTH: 11

YEAR: 2007

The highly permeable blood-brain barrier: an evaluation of current opinions about brain uptake capacity. Information

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LANGUAGE: eng

NlmUniqueID: 9604391

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AFFILIATION: Clinical Pharmacology, AstraZeneca R&D Södertälje, S-151 85 Södertälje, Sweden. urban.fagerholm@astrazeneca.com

Country: England

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MEDLINETA: Drug Discov Today

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