Kinetic studies of N-allenic analogues of tryptamine as monoamine oxidase inhibitors.
A series of N-allenic analogues of tryptamine in which the side chain is located at the 2 position of the indole ring, but which differed in the ring and side-chain nitrogen substituents, were assayed kinetically as MAO A and MAO B inhibitors. All the compounds studied were mechanism-based inhibitors. The kinetic constants of each inhibition step Ki and ki, were determined for both MAO A and B. The data obtained indicated that these allenic derivatives show a greater selectivity and potency towards MAO A as inhibitors than the corresponding acetylenic derivatives.
Perez
V
V
Depart. Bioquimica i Biologia Molecular Fac. Medicina, Universitat Autònoma de Barcelona, Spain.
Marco
J L
JL
Fernandez-Alvarez
E
E
Unzeta
M
M
D000818:Animals; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014363:Tryptamines / Q000494:pharmacology*
D008996:Monoamine Oxidase Inhibitors; D014363:Tryptamines