Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores.

作者: John M. Keith , Ann J. Barbier , Sandy J. Wilson , Kirstin Miller , Jamin D. Boggs

DOI: 10.1016/J.BMCL.2007.08.017

关键词:

摘要: A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H 3 antagonists is described. The introduction polar aromatic spacers part the histamine pharmacophore was explored. convergent synthesis final products allowing late stage side chain developed. In vitro and in vivo data are discussed.

参考文章(17)
John M. Zajecka, Clinical issues in long-term treatment with antidepressants. The Journal of Clinical Psychiatry. ,vol. 61, pp. 20- 25 ,(2000)
Nissar A. Darmani, Sharon L. Reeves, The stimulatory and inhibitory components of cocaine's actions on the 5-HTP-induced 5-HT2A receptor response Pharmacology, Biochemistry and Behavior. ,vol. 55, pp. 387- 396 ,(1996) , 10.1016/S0091-3057(96)00108-6
Esther Babad, Nicholas I. Carruthers, Robert S. Jaret, Martin Steinman, A Short Synthesis of Albuterol Synthesis. ,vol. 1988, pp. 966- 968 ,(1988) , 10.1055/S-1988-27768
Michael A. Letavic, John M. Keith, Jill A. Jablonowski, Emily M. Stocking, Leslie A. Gomez, Kiev S. Ly, Jennifer M. Miller, Ann J. Barbier, Pascal Bonaventure, Jamin D. Boggs, Sandy J. Wilson, Kirsten L. Miller, Brian Lord, Heather M. McAllister, D.J. Tognarelli, Jiejun Wu, Marta C. Abad, Carsten Schubert, Timothy W. Lovenberg, Nicholas I. Carruthers, Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorganic & Medicinal Chemistry Letters. ,vol. 17, pp. 1047- 1051 ,(2007) , 10.1016/J.BMCL.2006.11.036
Richard Apodaca, Curt A. Dvorak, Wei Xiao, Ann J. Barbier, Jamin D. Boggs, Sandy J. Wilson, Timothy W. Lovenberg, Nicholas I. Carruthers, A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. Journal of Medicinal Chemistry. ,vol. 46, pp. 3938- 3944 ,(2003) , 10.1021/JM030185V
Jaime M. Monti, Héctor Jantos, María Boussard, Humberto Allier, Cecilia Orellana, Silvia Olivera, Effects of selective activation or blockade of the histamine H3 receptor on sleep and wakefulness European Journal of Pharmacology. ,vol. 205, pp. 283- 287 ,(1991) , 10.1016/0014-2999(91)90911-9
Charles M. Beasley, Stephanie C. Koke, Mary E. Nilsson, Jill S. Gonzales, Adverse events and treatment discontinuations in clinical trials of fluoxetine in major depressive disorder : An updated meta-analysis Clinical Therapeutics. ,vol. 22, pp. 1319- 1330 ,(2000) , 10.1016/S0149-2918(00)83028-3
Michael A. Letavic, John M. Keith, Kiev S. Ly, Ann J. Barbier, Jamin D. Boggs, Sandy J. Wilson, Brian Lord, Timothy W. Lovenberg, Nicholas I. Carruthers, Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors. Bioorganic & Medicinal Chemistry Letters. ,vol. 17, pp. 2566- 2569 ,(2007) , 10.1016/J.BMCL.2007.02.006
Andrew A. Nierenberg, Bronwyn R. Keefe, Vinita C. Leslie, Jonathan E. Alpert, Joel A. Pava, John J. Worthington, Jerrold F. Rosenbaum, Maurizio Fava, Residual symptoms in depressed patients who respond acutely to fluoxetine. The Journal of Clinical Psychiatry. ,vol. 60, pp. 221- 225 ,(1999) , 10.4088/JCP.V60N0403
Eva Jané-Llopis, Clemens Hosman, Rachel Jenkins, Peter Anderson, Predictors of efficacy in depression prevention programmes: Meta-analysis British Journal of Psychiatry. ,vol. 183, pp. 384- 397 ,(2003) , 10.1192/BJP.183.5.384