Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors

SAR around a known molecule with dual 5-HT(1D) antagonist and 5-HT(transporter) inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT(1B), alpha(1), and D(2)).

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3344-3348
Hauptverfasser:	BUENO, Ana B, GILMORE, Jeremy, TIMMS, Graham, TOMLINSON, Rosemarie, WALLACE, Louise, WALTON, Leslie, BOOT, John, BROADMORE, Richard, COOPER, Jane, FINDLAY, Jeremy, HAYHURST, Lorna, MARCOS, Alicia, MONTERO, Carlos, MITCHELL, Stephen
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antidepressive Agents - chemical synthesis Antidepressive Agents - pharmacology Biological and medical sciences Dose-Response Relationship, Drug Guinea Pigs Kinetics Medical sciences Models, Chemical Naphthalenes - chemistry Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - pharmacology Receptor, Serotonin, 5-HT1D - drug effects Receptor, Serotonin, 5-HT1D - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacology Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - pharmacology Serotoninergic system Stereoisomerism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	SAR around a known molecule with dual 5-HT(1D) antagonist and 5-HT(transporter) inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT(1B), alpha(1), and D(2)).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.03.101