Novel azulene derivatives for the treatment of erectile dysfunction |
| |
Authors: | Stefan Löber Harald Hübner Armin Buschauer Fabrizio Sanna Antonio Argiolas Maria Rosaria Melis Peter Gmeiner |
| |
Institution: | 1. Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, Schuhstrasse 19, D-91052 Erlangen, Germany;2. Institut für Pharmazie, Universität Regensburg, D-93040 Regensburg, Germany;3. Department of Biomedical Sciences, Neuroscience and Clinical Pharmacology Section, University of Cagliari, S.S. 554, km 4500, 09042 Monserrato, Cagliari, Italy |
| |
Abstract: | Based on the dopamine D4 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 D4 partial agonist (EC50 = 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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|