Lack of hypotensive and brain catecholamine depleting effects by erythro- and threo-alpha-methyl DOPS.
An investigation was carried out to ascertain whether erythro- and threo-alpha-methyl-dihydroxy-phenyl-serine were able of depleting cerebral and peripheral norepinephrine (NE) through their metabolization to alpha-mNE. The results show that the alpha-methyl-aminoacids were decarboxylated only at the periphery and that the threo-form caused depletion in cardiac NE. In any case, both isomers were unable to cross the blood-brain barrier leaving the cerebral NE unaffected. Consequently the use of alpha-mDOPS as alternative tool to alpha-mDOPA in the therapy for hypertension seems unlikely to occur. The results also provide evidence for differences in the pharmacokinetics of the two isomers.
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D001923:Brain Chemistry / Q000187:drug effects*; D002395:Catecholamines / Q000378:metabolism*; D015103:Droxidopa / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004347:Drug Interactions; D051381:Rats; D012694:Serine / Q000031:analogs & derivatives*; D013997:Time Factors; D014443:Tyrosine / Q000097:blood
D002395:Catecholamines; D014443:Tyrosine; D012694:Serine; D015103:Droxidopa