system l transporter การใช้

However, after extensive searching it was discovered that one enantiomer of the relatively simple derivative 4-methylpregabalin, was both 4x higher in binding affinity to ? 2 ? channels than pregabalin, and also retained similar affinity for the system L transporter.
This explained the previous failures, as most alterations to the pregabalin molecule which increase affinity for the ? 2 ? channels and therefore increase apparent potency in the test tube, were found to also dramatically reduce binding to the system L transporter, and with no assisted transport into the brain, blood brain barrier penetration was minimal and the drugs were inactive in animals.