Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
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 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
Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. simon.e.ward@gsk.com
Johnson
Christopher N
CN
Lovell
Peter J
PJ
Scott
Claire M
CM
Smith
Paul W
PW
Stemp
Geoffrey
G
Thewlis
Kevin M
KM
Vong
Antonio K
AK
Watson
Jeannette M
JM
D000284:Administration, Oral; D001682:Biological Availability; D008024:Ligands; D011985:Receptors, Serotonin / Q000378:metabolism*; D018490:Serotonin Agents / Q000378:metabolism* / Q000493:pharmacokinetics
D008024:Ligands; D011985:Receptors, Serotonin; D018490:Serotonin Agents