Synthesis and Biological Investigations of Dopaminergic Partial Agonists Preferentially Recognizing the D4 Receptor Subtype

Löber S, Gmeiner P, Hübner H (2006)

Publication Type: Journal article

Publication year: 2006

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 16

Pages Range: 2955-2959

DOI: 10.1016/j.bmcl.2006.02.075

Abstract

Aminomethyl-substituted biaryls bearing a pyrazole or triazole moiety were synthesized and investigated for dopamine and serotonin receptor binding. The N-arylpyrazoles 3b,f,g and 4 revealed Ki values in the subnanomolar range (0.28-0.70 nM) for the dopamine D4 receptor subtype. Employing both mitogenesis and GTPγS assays, ligand efficacy was evaluated indicating partial agonist properties. Interestingly, the tetrahydropyrimidine 4 (FAUC 2020) displayed significant intrinsic selectivity for D2long over D2short. © 2006 Elsevier 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. (2006). Synthesis and Biological Investigations of Dopaminergic Partial Agonists Preferentially Recognizing the D4 Receptor Subtype. Bioorganic & Medicinal Chemistry Letters, 16, 2955-2959. https://doi.org/10.1016/j.bmcl.2006.02.075

MLA:

Löber, Stefan, Peter Gmeiner, and Harald Hübner. "Synthesis and Biological Investigations of Dopaminergic Partial Agonists Preferentially Recognizing the D4 Receptor Subtype." Bioorganic & Medicinal Chemistry Letters 16 (2006): 2955-2959.

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