Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands |
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| 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 |
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| Affiliation: | Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. simon.e.ward@gsk.com |
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| Abstract: | 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. |
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