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

Ward, Simon ORCID: https://orcid.org/0000-0002-8745-8377, Eddershaw, Peter, Flynn, Sean T., Gordon, Laurie, Lovell, Peter J., Moore, Susan H., Scott, Claire M., Smith, Paul W., Thewlis, Kevin M. and Wyman, Paul A. 2008. Studies on a series of potent, orally bioavailable, 5-HT1 receptor ligands-Part II. Biorganic and Medicinal Chemistry Letters 19 (2) , pp. 428-432. 10.1016/j.bmcl.2008.11.052

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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 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.

Item Type:	Article
Date Type:	Published Online
Status:	Published
Schools:	Schools > Medicine
Uncontrolled Keywords:	5-HT1, SSRI, Serotonin, 5-HT1A antagonist, Depression
Publisher:	Elsevier
ISSN:	0960-894X
Date of Acceptance:	14 November 2008
Last Modified:	23 Oct 2022 12:59
URI:	https://orca.cardiff.ac.uk/id/eprint/109348

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