Monoamine oxidase-A selective inhibition in human hypothalamus and liver in-vitro by amiflamine and its metabolites.
Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 microM (liver) and 0.8, 0.2 and 14 microM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds.
Tipton
K F
KF
O'Carroll
A M
AM
McCrodden
J M
JM
Fowler
C J
CJ
D000818:Animals; D006801:Humans; D007031:Hypothalamus / Q000201:enzymology*; D066298:In Vitro Techniques; D007700:Kinetics; D008099:Liver / Q000201:enzymology*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010627:Phenethylamines / Q000494:pharmacology*; D051381:Rats
D008996:Monoamine Oxidase Inhibitors; D010627:Phenethylamines; C031466:amiflamine