892403-81-5Relevant articles and documents
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore
Keith, John M.,Gomez, Leslie A.,Letavic, Michael A.,Ly, Kiev S.,Jablonowski, Jill A.,Seierstad, Mark,Barbier, Ann J.,Wilson, Sandy J.,Boggs, Jamin D.,Fraser, Ian C.,Mazur, Curt,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 702 - 706 (2007/10/03)
A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors
Letavic, Michael A.,Keith, John M.,Jablonowski, Jill A.,Stocking, Emily M.,Gomez, Leslie A.,Ly, Kiev S.,Miller, Jennifer M.,Barbier, Ann J.,Bonaventure, Pascal,Boggs, Jamin D.,Wilson, Sandy J.,Miller, Kirsten L.,Lord, Brian,McAllister, Heather M.,Tognarelli,Wu, Jiejun,Abad, Marta C.,Schubert, Carsten,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 1047 - 1051 (2007/10/03)
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H3 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.
TETRAHYDROISOQUINOLINE COMPOUNDS FOR TREATMENT OF CNS DISORDERS
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Page/Page column 55-56, (2010/11/08)
Certain tetrahydroisoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor-and serotonin-mediated diseases.