An in vitro Model for Blood Brain Barrier Permeation
1
Institute of Pharmaceutical Chemistry, University of Vienna, A-1090 Wien, Austria
2
Institute of Pharmaceutical Chemistry, Johm-Wolfgang-Goethe University, Frankfurt/Main, Germany
3
Institute of Biochemistry and Molecular Cell Biology, University of Vienna, A- 1030 Wien, Austria
4
Institute of Physical Chemistry, University of Vienna, A-1090 Wien, Austria
5
Institute of Biochemistry, Technical University Darmstadt, D-64287 Darmstadt, Germany
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2002, 70(4), 317-322; https://doi.org/10.3797/scipharm.aut-02-30
Submission received: 30 October 2002
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Revised: 20 November 2002
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Accepted: 20 November 2002
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Published: 22 November 2002
Abstract
The ability to permeate accross the blood brain barrier (BBB) is essential for drugs acting on the central nervous system (CNS). Thus, systems that allow rapid and inexpensive screening of the BBB-permeability properties of novel lead compounds are of great importance for speeding up the drug discovery process in the CNS-area. We used immortalized porcine brain microvessel endothelial cells (PBMECICl-2) to develop a model for measurement of blood-brain barrier permeation of CNS active drugs. Investigation of different cell culture conditions showed, that a system using C6 astrocyte glioma conditioned medium and addition of a cyclic AMP analog in combination with a type IV phosphodiesterase inhibitor (R020-1724) leads to cell layers with transendothelial electrical resistance values up to 300 Ω.cm2. Permeability studies with U-[14C]sucroseg ave a permeability coefficient Pe of 3.24 + 0.14 × 10−4 cm/min, which is in good agreement to published values and thus indicates the formation of tight junctions in vitro.
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MDPI and ACS Style
R., B.; R., L.; B., L.; F., P.; G.A., P.; G.F., E.; P., F.; C.R., N. An in vitro Model for Blood Brain Barrier Permeation. Sci. Pharm. 2002, 70, 317-322. https://doi.org/10.3797/scipharm.aut-02-30
AMA Style
R. B, R. L, B. L, F. P, G.A. P, G.F. E, P. F, C.R. N. An in vitro Model for Blood Brain Barrier Permeation. Scientia Pharmaceutica. 2002; 70(4):317-322. https://doi.org/10.3797/scipharm.aut-02-30
Chicago/Turabian StyleR., Bauer, Lauer R., Linz B., Pittner F., Peschek G.A., Ecker G.F., Friedl P., and Noe C.R. 2002. "An in vitro Model for Blood Brain Barrier Permeation" Scientia Pharmaceutica 70, no. 4: 317-322. https://doi.org/10.3797/scipharm.aut-02-30
