Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.
A series of 5-(piperidinylethyloxy)quinoline 5-HT(1) receptor ligands have been studied by elaboration of the series of dual 5-HT(1)-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.
Ward
Simon E
SE
Neuroscience Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. simon.e.ward@gsk.com
Eddershaw
Peter
P
Flynn
Sean T
ST
Gordon
Laurie
L
Lovell
Peter J
PJ
Moore
Susan H
SH
Scott
Claire M
CM
Smith
Paul W
PW
Thewlis
Kevin M
KM
Wyman
Paul A
PA
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D008024:Ligands; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D044263:Receptors, Serotonin, 5-HT1 / Q000187:drug effects*; D013329:Structure-Activity Relationship
D008024:Ligands; D011804:Quinolines; D044263:Receptors, Serotonin, 5-HT1