PCP, like ketamine, also acts as a D 2 receptor partial agonist in rat brain homogenate This activity may be associated with some of the other more psychotic features of PCP intoxication, which is evidenced by the successful use of D2 receptor antagonists ( such as haloperidol ) in the treatment of PCP psychosis.
42.
HxA3 was converted through a Michael addition catalyzed by glutathione transferase to its glutathione conjugate, HxA3-C, i . e ., 11-glutathionyl-HxA3, in a cell-free system or in homogenates of rat brain hippocampus tissue; HxA3-C proved to be a potent stimulator of membrane hyperpolarization in rat hippocampal CA1 neurons.
43.
Opicapone showed to have a stronger and more sustained COMT inhibitory effect than the comparing COMT inhibitors tolcapone and entacapone : in liver and brain homogenates from rats administered with opicapone, tolcapone and entacapone by gastric tube, one hour after administration, COMT inhibition was 99 % with opicapone versus 82 % with tolcapone and 68 % with entacapone; nine hours after administration, entacapone showed no COMT inhibition and tolcapone produced minimal inhibitory effect ( 16 % ), whereas opicapone continued to inhibit COMT activity by 91 %.
