Transport mechanisms of opioid analgesics across the blood-brain barrier

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An organic cation/proton antiporter is involved in the CNS acting cationic drug transport in the human blood-brain barrier model cells, suggesting that the proton antiporter mediates oxycodone transport into the brain across the blood-brain barrier in humans as well as rodents. Further, we showed that functions of organic cation-related transporters are able to be suppressed by small interfering RNA (siRNA). The siRNA screening method should be useful for the identification of the proton antiporter molecule which mediates blood-to-brain transport of oxycodone.