5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.

Abstract 5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1 H )-quinolinones and 3,4-dihydro-2(1 H )-quinolinones have been identified with different combinations of 5-HT 1 autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of profiles at targets known to play a key role in the control of synaptic 5-HT levels will allow exploration of different pharmacological profiles in a range of animal behavioral and disease models.