2,4-Disubstituted Pyrroles: Synthesis, Traceless Linking and Pharmacological Investigations Leading to the Dopamine D4 Receptor Partial Agonist FAUC 356

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: 1937-1940

DOI: 10.1016/S0960-894X(02)00316-5

Abstract

Solution-phase synthesis and a solid-phase supported approach to piperazinylmethyl substituted pyrroles are described. Receptor binding studies and the measurement of D4 ligand efficacy led to the ethynylpyrrole 1d (FAUC 356) exerting selective D4 binding and substantial ligand efficacy (66%, EC50=1.9 nM). This activity profile might be of interest for the treatment of ADHD. © 2002 Elsevier Science Ltd. All rights reserved.

Authors with CRIS profile

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

How to cite

APA:

Gmeiner, P., & Hübner, H. (2002). 2,4-Disubstituted Pyrroles: Synthesis, Traceless Linking and Pharmacological Investigations Leading to the Dopamine D4 Receptor Partial Agonist FAUC 356. Bioorganic & Medicinal Chemistry Letters, 12, 1937-1940. https://doi.org/10.1016/S0960-894X(02)00316-5

MLA:

Gmeiner, Peter, and Harald Hübner. "2,4-Disubstituted Pyrroles: Synthesis, Traceless Linking and Pharmacological Investigations Leading to the Dopamine D4 Receptor Partial Agonist FAUC 356." Bioorganic & Medicinal Chemistry Letters 12 (2002): 1937-1940.

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