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

Ward, Simon, Johnson, Christopher N., Lovell, Peter J., Scott, Claire M., Smith, Paul W., Stemp, Geoffrey, Thewlis, Kevin M., Vong, Antonio K. and Watson, Jeannette M. 2007. Studies on a series of potent, orally bioavailable, 5-HT1 receptor ligands. Biorganic and Medicinal Chemistry Letters 17 (18) , pp. 5214-5217. 10.1016/j.bmcl.2007.06.078

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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 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.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Uncontrolled Keywords: 5-HT, Serotonin, Depression, Autoreceptors
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 27 June 2007
Last Modified: 28 Feb 2018 11:43

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