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

Ward, Simon ORCID: https://orcid.org/0000-0002-8745-8377, 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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Abstract

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:	23 Oct 2022 13:00
URI:	https://orca.cardiff.ac.uk/id/eprint/109402

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