Synthesis and Dopamine Receptor Binding Studies of Homochiral 8-Aminopyrido[1,2-a]indoles

Gmeiner P (1995)


Publication Type: Journal article

Publication year: 1995

Journal

Publisher: Wiley-VCH Verlag

Book Volume: 328

Pages Range: 626-628

DOI: 10.1002/ardp.19953280712

Abstract

Starting from L-aspartic acid the preparation of 8-aminopyrido[1,2-a]indole derivatives as benzo-fused analogs of the dopamine autoreceptor agonist 1 is reported. The key step of the synthesis is the Tf2O induced cyclization of the 1,2-amino alcohol 6. Receptor binding studies indicated selective affinity for the D-2 autoreceptor. Among the tested compounds, the dipropylamino derivative 2 showed the highest affinity for the D-2 receptor labelled with the selective autoreceptor agonist pramipexole (IC50 value: 450 nM). Thus, 2 is 15 times less potent than the aminoindolizine 1.

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How to cite

APA:

Gmeiner, P. (1995). Synthesis and Dopamine Receptor Binding Studies of Homochiral 8-Aminopyrido[1,2-a]indoles. Archiv Der Pharmazie, 328, 626-628. https://doi.org/10.1002/ardp.19953280712

MLA:

Gmeiner, Peter. "Synthesis and Dopamine Receptor Binding Studies of Homochiral 8-Aminopyrido[1,2-a]indoles." Archiv Der Pharmazie 328 (1995): 626-628.

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