Fancy Bioisosteres: Metallocene-Derived G-Protein-Coupled Receptor Ligands with Subnanomolar Binding Affinity and Novel Selectivity Profiles

Gmeiner P, Hübner H (2005)


Publication Type: Journal article

Publication year: 2005

Journal

Publisher: American Chemical Society

Book Volume: 48

Pages Range: 3696-3699

DOI: 10.1021/jm050170s

Abstract

Metallocene-derived bioisosteres lead to exceptionally strong binding G-protein-coupled receptor ligands, indicating substantial plasticity of the receptor excluded volume. Novel binding profiles of ferrocenylcarboxamides combining subnanomolar Ki values for the dopamine D4 receptor (1a, 0.52 nM; 1b, 0.63 nM) with superpotent serotonin 5-hydroxytryptamine 1A (1a, 0.50 nM) and dopamine D3 receptor binding (1b, 0.64 nM) and selective D4 agonist properties of the ruthenocene 1c may be a starting point for highly beneficial central nervous system active drugs. © 2005 American Chemical Society.

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How to cite

APA:

Gmeiner, P., & Hübner, H. (2005). Fancy Bioisosteres: Metallocene-Derived G-Protein-Coupled Receptor Ligands with Subnanomolar Binding Affinity and Novel Selectivity Profiles. Journal of Medicinal Chemistry, 48, 3696-3699. https://doi.org/10.1021/jm050170s

MLA:

Gmeiner, Peter, and Harald Hübner. "Fancy Bioisosteres: Metallocene-Derived G-Protein-Coupled Receptor Ligands with Subnanomolar Binding Affinity and Novel Selectivity Profiles." Journal of Medicinal Chemistry 48 (2005): 3696-3699.

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