Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors

A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (4), p.1047-1051
Hauptverfasser:	LETAVIC, Michael A, KEITH, John M, WILSON, Sandy J, MILLER, Kirsten L, LORD, Brian, MCALLISTER, Heather M, TOGNARELLI, D. J, JIEJUN WU, ABAD, Marta C, SCHUBERT, Carsten, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I, JABLONOWSKI, Jill A, STOCKING, Emily M, GOMEZ, Leslie A, LY, Kiev S, MILLER, Jennifer M, BARBIER, Ann J, BONAVENTURE, Pascal, BOGGS, Jamin D
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Crystallography, X-Ray Dopamine Plasma Membrane Transport Proteins - drug effects Dopamine Plasma Membrane Transport Proteins - metabolism Half-Life Histamine Antagonists - chemical synthesis Histamine Antagonists - pharmacology Humans Indicators and Reagents Medical sciences Models, Molecular Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Norepinephrine - metabolism Pharmacology. Drug treatments Rats Receptors, Histamine H3 - drug effects Serotonin Plasma Membrane Transport Proteins - drug effects Serotonin Plasma Membrane Transport Proteins - metabolism Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - pharmacokinetics Serotonin Uptake Inhibitors - pharmacology Serotoninergic system Structure-Activity Relationship Tetrahydroisoquinolines - chemical synthesis Tetrahydroisoquinolines - pharmacokinetics Tetrahydroisoquinolines - pharmacology
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Beschreibung
Zusammenfassung:	A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.11.036