Dopaminergic 7-Aminotetrahydroindolizines: Ex-Chiral Pool Synthesis and Preferential D3 Receptor Binding

Gmeiner P, Hübner H (2001)

Publication Type: Journal article

Publication year: 2001

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 11

Pages Range: 2863-2866

DOI: 10.1016/S0960-894X(01)00564-9

Abstract

Starting from both isomers of enantiopure asparagine, heterocyclic bioisosteres of the preferential dopamine D3 receptor agonist (R)-7-OH-DPAT were investigated when SAR studies led to the 3-formyl substituted aminoindolizine (S)-1e (FAUC 54) displaying a K(i) value of 6.0 nM for the high affinity D3 binding site. In contrast, D3 affinity of the enantiomer (R)-1e was 300 fold lower.

Authors with CRIS profile

Peter Gmeiner Lehrstuhl für Pharmazeutische Chemie Harald Hübner Lehrstuhl für Pharmazeutische Chemie

How to cite

APA:

Gmeiner, P., & Hübner, H. (2001). Dopaminergic 7-Aminotetrahydroindolizines: Ex-Chiral Pool Synthesis and Preferential D3 Receptor Binding. Bioorganic & Medicinal Chemistry Letters, 11, 2863-2866. https://doi.org/10.1016/S0960-894X(01)00564-9

MLA:

Gmeiner, Peter, and Harald Hübner. "Dopaminergic 7-Aminotetrahydroindolizines: Ex-Chiral Pool Synthesis and Preferential D3 Receptor Binding." Bioorganic & Medicinal Chemistry Letters 11 (2001): 2863-2866.

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