Article ID Journal Published Year Pages File Type
2562962 Pharmacological Research 2007 7 Pages PDF
Abstract

PurposeThe objective of the current study was to determine the ability of some antiemetic compounds to cross the blood–brain barrier (BBB) and thereby to determine possible side effects of compounds for the central nervous system (CNS).MethodsWe compared the brain penetration of some antiemetic compounds using an in vitro BBB model consisting in brain capillary endothelial cells co-cultured with primary rat glial cells.ResultsThis study clearly demonstrated that the metopimazine metabolite, metopimazine acid, has a very low brain penetration, lower than metopimazine and even less than the other antiemetic compounds tested in this study.ConclusionsThe poor brain penetration of metopimazine acid, metopimazine biodisponible form, seems very likely related to the clinically observed difference in therapeutic and safety profile.

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