Penetration of some O-and/or N-methylated norepinephrine derivatives through the rat blood brain barrier.
Methods for the determination of a number of O and/or N-methylated derivatives of norepinephrine were developed. The IP injection of these compounds into rats shows quick absorption and short half-lives in plasma, liver and brain. Most compounds do not cross the Blood-Brain-Barrier (BBB) due to low lipid solubility. However, lipid solubility is not a sole determinant. Compounds which have at least one of the 2 phenolic hydroxyl groups methylated and possess a tertiary amino group do cross the BBB readily.
D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D008055:Lipids; D008099:Liver / Q000378:metabolism; D008297:Male; D008745:Methylation; D009638:Norepinephrine / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism; D051381:Rats; D012995:Solubility; D013329:Structure-Activity Relationship; D013997:Time Factors
D008055:Lipids; D009638:Norepinephrine