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.
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-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.
Bromidge
Steven M
SM
Neurosciences CEDD, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. steven.bromidge@evotec.com
Arban
Roberto
R
Bertani
Barbara
B
Borriello
Manuela
M
Capelli
Anna-Maria
AM
Di-Fabio
Romano
R
Faedo
Stefania
S
Gianotti
Massimo
M
Gordon
Laurie J
LJ
Granci
Enrica
E
Pasquarello
Alessandra
A
Spada
Simone K
SK
Worby
Angela
A
Zonzini
Laura
L
Zucchelli
Valeria
V
D000818:Animals; D017660:Autoreceptors / Q000037:antagonists & inhibitors / Q000187:drug effects; D015363:Quinolones / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D044263:Receptors, Serotonin, 5-HT1 / Q000187:drug effects*; D017367:Selective Serotonin Reuptake Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D013569:Synapses / Q000737:chemistry
D017660:Autoreceptors; D015363:Quinolones; D044263:Receptors, Serotonin, 5-HT1; D017367:Selective Serotonin Reuptake Inhibitors