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. 2020 Jan 9;63(3):1361–1387. doi: 10.1021/acs.jmedchem.9b01886

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
a

Data are mean values ± SD (n = 1, in triplicate). nd, not determined.

b

In vitro: 50 μM compounds (final concentrations) versus 0.9% saline with mouse brain homogenate from nontreated mice.

c

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.