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Bioorg Med Chem Lett. 2009 Jan 15;19(2):428-32. doi: 10.1016/j.bmcl.2008.11.052. Epub 2008 Nov 19.

Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.

Author information

1
Neuroscience Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. simon.e.ward@gsk.com

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 in vitro 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.

PMID:
19071020
DOI:
10.1016/j.bmcl.2008.11.052
[Indexed for MEDLINE]

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