Studies on a series of potent, orally bioavailable, 5-HT1 receptor ligands—Part II

A series of 5-(piperidinylethyloxy)quinoline 5-HT1 receptor ligands have been studied by elaboration of the series of dual 5-HT1-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT1A, 5-HT1B and 5-HT1D receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.

SAR studies on a series of substituted phenyl piperazines and piperidines are described. Several examples are disclosed as potent 5-HT1 receptor ligands and their PK profiles presented.Figure optionsDownload as PowerPoint slide