Discovery of dopamine D4 receptor antagonists with planar chirality

Sanna F, Ortner B, Hübner H, Löber S, Tschammer N, Gmeiner P (2013)

Publication Language: English

Publication Type: Journal article, Original article

Publication year: 2013

Journal

Original Authors: Sanna F., Ortner B., Hubner H., Lober S., Tschammer N., Gmeiner P.

Publisher: Elsevier

Book Volume: 21

Pages Range: 1680-1684

Journal Issue: 7

DOI: 10.1016/j.bmc.2013.01.065

Abstract

Employing the D selective phenylpiperazine 2 as a lead compound, planar chiral analogs with paracyclophane substructure were synthesized and evaluated for their ability to bind and activate dopamine receptors. The study revealed that the introduction of a [2.2]paracyclophane moiety is tolerated by dopamine receptors of the D family. Subtype selectivity for D and ligand efficacy depend on the absolute configuration of the test compounds. Whereas the achiral single-layered lead 2 and the double-layered paracyclophane (R)-3 showed partial agonist properties, the enantiomer (S)-3 behaved as a neutral antagonist. © 2013 Elsevier Ltd. All rights reserved.

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APA:

Sanna, F., Ortner, B., Hübner, H., Löber, S., Tschammer, N., & Gmeiner, P. (2013). Discovery of dopamine D4 receptor antagonists with planar chirality. Bioorganic & Medicinal Chemistry, 21(7), 1680-1684. https://dx.doi.org/10.1016/j.bmc.2013.01.065

MLA:

Sanna, Fabrizio, et al. "Discovery of dopamine D4 receptor antagonists with planar chirality." Bioorganic & Medicinal Chemistry 21.7 (2013): 1680-1684.

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