The Blood-Brain Barrier (BBB), the most limiting barrier in the body, consists of a continuous monolayer of endothelial cells that lines the inner surface of the capillaries, delimiting and separating the brain from the bloodstream.

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For CNS action compounds, penetration of this monolayer is essential, however in compounds targeting peripheral sites, penetration must be minimized in order to reduce potential adverse effects.

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Thus, studies of BBB-Drug intercations are crucial too understand if the compound passes through this barrier and what its influence on the constituent membranes of the BBB cells.