Studies on 5-fluoro-alpha-methyltryptamine and p-chloro-beta-methylphenethylamine: determination of the MAO-A or MAO-B selective inhibition in vitro.
To further clarify highly MAO-A- or -B-selective inhibitory properties of 5-fluoro-alpha-methyltryptamine (5-FMT) and p-chloro-beta-methylphenethylamine (p-CMPEA), we determined the types and K1 values of inhibition of rat brain MAO-A and -B activity in vitro. The kinetic data obtained showed that 5-FMT is a competitive MAO-A-selective inhibitor with about a 18,000-fold higher sensitivity than MAO-B. In contrast, p-CMPEA is a competitive MAO-B-selective inhibitor with about a 620-fold higher sensitivity. Based on the present findings of highly MAO-A- or -B-selective inhibition, these two compounds might prove to be of value in in vivo studies.
Kinemuchi
H
H
Department of Pharmacology, School of Medicine, Showa University, Tokyo, Japan.
Arai
Y
Y
Toyoshima
Y
Y
Tadano
T
T
Kisara
K
K
D000662:Amphetamines / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000201:enzymology*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D014363:Tryptamines / Q000494:pharmacology*; D010133:p-Chloroamphetamine / Q000031:analogs & derivatives / Q000494:pharmacology*
D000662:Amphetamines; D008996:Monoamine Oxidase Inhibitors; D014363:Tryptamines; C051100:4-chloro-beta-methylphenethylamine; D010133:p-Chloroamphetamine; C051101:5-fluoro-alpha-methyltryptamine