Brofaromine (CGP 11305A) is a monoamine oxidase (MAO) inhibitor with IC50 of 0.2 μM for MAO-A.
In order to assess whether the protective effect is related to the inhibition of the MAO-A or due to another mechanism, the effect of Brofaromine (CGP 11305A, BRO) is determined on the activity of MAO-A in cultured cortical cells. It shows, firstly, that cultured cortical cells have a significant MAO-A activity, and secondly, that Brofaromine inhibits the enzyme in a concentration-dependent manner. The IC50 is 0.19 μM for Brofaromine . Hill coefficient is 0.96. The enzyme is almost completely inhibited at 10 μM . Brofaromine inhibits MAO-A activity of our cultured cortical cells in a concentration-dependent manner. The IC50 range of Brofaromine is 0.01 μM to 0.1 μM[1].
[1]. Boland A, et al. Pirlindole and dehydropirlindole protect rat cultured neuronal cells against oxidative stress-induced cell death through a mechanism unrelated to MAO-A inhibition. Br J Pharmacol. 2002 Feb;135(3):713-20.