Novel azulene derivatives for the treatment of erectile dysfunction
Löber S, Hübner H, Buschauer A, Sanna F, Argiolas A, Melis MR, Gmeiner P (2012)
Publication Language: English
Publication Type: Journal article, Original article
Publication year: 2012
Journal
Original Authors: Lober S., Hubner H., Buschauer A., Sanna F., Argiolas A., Melis M.R., Gmeiner P.
Publisher: Elsevier
Book Volume: 22
Pages Range: 7151-7154
Journal Issue: 23
DOI: 10.1016/j.bmcl.2012.09.064
Abstract
Based on the dopamine D receptor partial agonist FAUC 3019, a series of azulenylmethylpiperazines was synthesized and affinities for the monoaminergic GPCRs including dopamine, serotonin, histamine and α-adrenergic receptor subtypes were determined. Ligand efficacies of the most promising test compounds revealed the N,N-dimethylaminomethyl substituted azulene 11 to be the most potent D partial agonist (EC = 0.41 nM). This candidate was investigated for its ability to promote penile erection. Applying an in vivo animal model, test compound 11 turned out to stimulate penile erection in male rats with superior potency in low concentrations when compared to apomorphine. © 2012 Elsevier Ltd. All rights reserved.
Authors with CRIS profile
Stefan Löber
Lehrstuhl für Pharmazeutische Chemie
Harald Hübner
Lehrstuhl für Pharmazeutische Chemie
Peter Gmeiner
Lehrstuhl für Pharmazeutische Chemie
Additional Organisation(s)
Involved external institutions
Germany (DE)
Italy (IT)How to cite
APA:
Löber, S., Hübner, H., Buschauer, A., Sanna, F., Argiolas, A., Melis, M.R., & Gmeiner, P. (2012). Novel azulene derivatives for the treatment of erectile dysfunction. Bioorganic & Medicinal Chemistry Letters, 22(23), 7151-7154. https://dx.doi.org/10.1016/j.bmcl.2012.09.064
MLA:
Löber, Stefan, et al. "Novel azulene derivatives for the treatment of erectile dysfunction." Bioorganic & Medicinal Chemistry Letters 22.23 (2012): 7151-7154.
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