Different stereoselective inhibition of monoamine oxidase-B by the R- and S-enantiomers of MD 780236.
MD 780236, a selective inhibitor of the B form of MAO behaves as an irreversible inhibitor in in-vitro conditions and mainly as a short-acting inhibitor in ex-vivo experiments. The enantiomer with the R absolute configuration (MD 240928) is fully reversible in ex-vivo conditions, whereas the S-enantiomer (MD 240931) has kept the irreversible component of the inhibition seen with MD 780236. The corresponding racemic alcohol derivative (MD 760548) is also a short-acting inhibitor of the B form of MAO; its S-enantiomer, which has an absolute configuration corresponding to that of MD 240928, has a selectivity towards the B form superior to that of the other enantiomer. The mechanism of the MAO inhibition by MD 780236 is discussed.
D000818:Animals; D001711:Biotransformation; D001921:Brain / Q000201:enzymology; D066298:In Vitro Techniques; D007536:Isomerism; D008099:Liver / Q000201:enzymology; D008297:Male; D008996:Monoamine Oxidase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D010080:Oxazoles / Q000494:pharmacology*; D023303:Oxazolidinones; D051381:Rats; D011919:Rats, Inbred Strains
D008996:Monoamine Oxidase Inhibitors; D010080:Oxazoles; D023303:Oxazolidinones; C037871:MD 780236