Carbenoxolone does not cross the blood brain barrier: an HPLC study

Carbenoxolone (CBX) is a widely used gap junctional blocker. Considering several reports indicating that transient gap junctional blockade could be a favourable intervention following injuries to central nervous tissue, and some current enthusiasm in studies using systemic injections of CBX, it is i...

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Bibliographic Details
Published in:BMC neuroscience 2006-01, Vol.7 (1), p.3-3, Article 3
Main Authors: Leshchenko, Yevgen, Likhodii, Sergei, Yue, Wendy, Burnham, William M, Perez Velazquez, Jose L
Format: Article
Language:English
Subjects:
Animals
Blood-Brain Barrier
Carbenoxolone - administration & dosage
Carbenoxolone - blood
Carbenoxolone - cerebrospinal fluid
Carbenoxolone - pharmacokinetics
Chromatography, High Pressure Liquid
Injections, Intraperitoneal
Male
Osmolar Concentration
Rats
Rats, Long-Evans
Time Factors
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Summary:Carbenoxolone (CBX) is a widely used gap junctional blocker. Considering several reports indicating that transient gap junctional blockade could be a favourable intervention following injuries to central nervous tissue, and some current enthusiasm in studies using systemic injections of CBX, it is imperative to consider the penetration of CBX into central nervous tissue after systemic administrations. So far, only very indirect evidence suggests that CBX penetrates into the central nervous system after systemic administrations. We thus determined the amounts of CBX present in the blood and the cerebrospinal fluid of rats after intraperitoneal administration, using high performance liquid chromatography. CBX was found in the blood of the animals, up to 90 minutes post-injection. However, the cerebrospinal fluid concentration of CBX was negligible. Thus, we conclude that, most likely, CBX does not penetrate the blood brain barrier and therefore recommend careful consideration in the manner of administration, when a central effect is desired.
ISSN:1471-2202
1471-2202
DOI:10.1186/1471-2202-7-3