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 an...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-09, Vol.17 (18), p.5214-5217
Main Authors: Ward, Simon E, Johnson, Christopher N, Lovell, Peter J, Scott, Claire M, Smith, Paul W, Stemp, Geoffrey, Thewlis, Kevin M, Vong, Antonio K, Watson, Jeannette M
Format: Article
Language:English
Subjects:
Administration, Oral
Biological Availability
Ligands
Receptors, Serotonin - metabolism
Serotonin Agents - metabolism
Serotonin Agents - pharmacokinetics
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Summary: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.
ISSN:0960-894X
1464-3405