Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors

A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4374-4377
Main Authors: KEITH, John M, GOMEZ, Leslie A, BARBIER, Ann J, WILSON, Sandy J, BOGGS, Jamin D, LORD, Brian, MAZUR, Curt, ALUISIO, Leah, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Blood-Brain Barrier
Histamine H1 Antagonists - chemistry
Histamine H1 Antagonists - pharmacology
Medical sciences
Mice
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyrrolidines - chemistry
Pyrrolidines - pharmacology
Receptors, Histamine H3 - drug effects
Serotonin Plasma Membrane Transport Proteins - drug effects
Serotoninergic system
Structure-Activity Relationship
Tetrahydroisoquinolines - chemistry
Tetrahydroisoquinolines - pharmacology
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Description
Summary:A series of novel and potent 6-heteroaryl-pyrrolidino-tetrahydroisoquinolines with dual histamine H(3) antagonist/serotonin transporter inhibitor activity is described. In vitro and in vivo data are discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.03.043