Table 3. In Vitro and ex Vivo Mouse Brain Homogenate Residual Activities of 69 and 100 at 60 mg/kg ip on MAO-A and MAO-B According to Substratea.
| residual activity (%) |
||||||
|---|---|---|---|---|---|---|
| MAO-A substrate | MAO-A/B substrate | MAO-B substrate | ||||
| 5-HT (0.25 mM) | p-tyramine (0.5 mM) | benzylamine (0.5 mM) | ||||
| compd | in vitrob | ex vivoc | in vitrob | ex vivoc | in vitrob | ex vivoc |
| 69 | –1.3 ± 0.1 | 1.6 ± 0.02 | 31.3 ± 0.2 | 14.2 ± 0.2 | nd | nd |
| 100 | nd | nd | 59.4 ± 0.2 | 77.2 ± 0.2 | –7.7 ± 0.2 | 24.3 ± 0.5 |
Data are mean values ± SD (n = 1, in triplicate). nd, not determined.
In vitro: 50 μM compounds (final concentrations) versus 0.9% saline with mouse brain homogenate from nontreated mice.
Ex vivo: brain homogenates from mice treated (n = 3, per group) with 60 mg/kg ip compounds or 0.9% saline 30 min before brain homogenate preparation.