Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing

Troschütz R, Gmeiner P, Hübner H (2004)

Publication Type: Journal article

Publication year: 2004

Journal

Bioorganic & Medicinal Chemistry Elsevier

Publisher: Elsevier

Book Volume: 12

Pages Range: 2625-2637

Journal Issue: 10

DOI: 10.1016/j.bmc.2004.03.023

Abstract

Novel 4-arylpiperazin-1-yl-substituted 2,3-dihydro-1H-1,4- and 1H-1,5-benzodiazepines and their aza-analogues were synthesized as debenzoclozapine derivatives for evaluation as potential D4-ligands. While Ki values of some of the title compounds came within the range of clozapine, they showed an impressively greater selectivity over other dopamine receptor subtypes, especially D2. For the most promising compounds, intrinsic activity and binding properties to serotonin 5-HT1A and 5-HT2 were also determined. © 2004 Elsevier Ltd. All rights reserved.

Authors with CRIS profile

Reinhard Troschütz Naturwissenschaftliche Fakultät Peter Gmeiner Lehrstuhl für Pharmazeutische Chemie Harald Hübner Lehrstuhl für Pharmazeutische Chemie

How to cite

APA:

Troschütz, R., Gmeiner, P., & Hübner, H. (2004). Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing. Bioorganic & Medicinal Chemistry, 12(10), 2625-2637. https://doi.org/10.1016/j.bmc.2004.03.023

MLA:

Troschütz, Reinhard, Peter Gmeiner, and Harald Hübner. "Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing." Bioorganic & Medicinal Chemistry 12.10 (2004): 2625-2637.

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