Di- and Trisubstituted Pyrazolo[1,5-a]pyridine Derivatives: Synthesis, Dopamine Receptor Binding and Ligand Efficacy

Löber S, Gmeiner P, Hübner H (2002)

Publication Type: Journal article

Publication year: 2002

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 12

Pages Range: 633-636

DOI: 10.1016/S0960-894X(01)00814-9

Abstract

Based on the lead molecule FAUC 113, a series of di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their dopamine receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (Ki = 1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC50 = 1.5 nM). © 2002 Elsevier Science Ltd. All rights reserved.

Authors with CRIS profile

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

How to cite

APA:

Löber, S., Gmeiner, P., & Hübner, H. (2002). Di- and Trisubstituted Pyrazolo[1,5-a]pyridine Derivatives: Synthesis, Dopamine Receptor Binding and Ligand Efficacy. Bioorganic & Medicinal Chemistry Letters, 12, 633-636. https://doi.org/10.1016/S0960-894X(01)00814-9

MLA:

Löber, Stefan, Peter Gmeiner, and Harald Hübner. "Di- and Trisubstituted Pyrazolo[1,5-a]pyridine Derivatives: Synthesis, Dopamine Receptor Binding and Ligand Efficacy." Bioorganic & Medicinal Chemistry Letters 12 (2002): 633-636.

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