Pharmacological research · 2006
Evidence of lowest brain penetration of an antiemetic drug, metopimazine, compared to domperidone, metoclopramide and chlorpromazine, using an in vitro model of the blood-brain barrier.
Сравнительное исследованиеСтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Jolliet Pascale, Nion Stéphane, Allain-Veyrac Gwenaëlle, Tilloy-Fenart L, Vanuxeem Dorothée, Berezowski Vincent, Cecchelli Roméo
Аннотация
PURPOSE: The 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).
METHODS: We 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.
RESULTS: This 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.
CONCLUSIONS: The poor brain penetration of metopimazine acid, metopimazine biodisponible form, seems very likely related to the clinically observed difference in therapeutic and safety profile.
METHODS: We 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.
RESULTS: This 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.
CONCLUSIONS: The poor brain penetration of metopimazine acid, metopimazine biodisponible form, seems very likely related to the clinically observed difference in therapeutic and safety profile.
Предметные рубрики MeSH
AnimalsAnimals, NewbornAntiemeticsBlood-Brain BarrierBrainCapillary PermeabilityCells, CulturedChlorpromazineClaudin-1Coculture TechniquesDomperidoneEndothelial CellsEndothelium, VascularIsonipecotic AcidsMembrane ProteinsMetoclopramideNeurogliaOccludinPhosphoproteinsRatsSucroseTight JunctionsZonula Occludens-1 Protein