Penetration of some O-and/or N-methylated norepinephrine derivatives through the rat blood brain barrier
Evans, B.D.; Vogel, W.H.
Research Communications in Chemical Pathology and Pharmacology 17(1): 61-76
1977
ISSN/ISBN: 0034-5164 PMID: 877406 Document Number: 122809
Methods for determination of a number of O and/or N-methylated derivatives of norepinephrine were developed. The i.p. 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, but lipid solubility is not a sole determinant. Compounds which have at least 1 of the 2 phenolic hydroxyl groups methylated and possess a tertiary amino group do cross the BBB readily.