Löber, Stefan and Hübner, Harald and Buschauer, Armin and Sanna, Fabrizio and Argiolas, Antonio and Melis, Maria Rosaria and Gmeiner, Peter (2012) Novel azulene derivatives for the treatment of erectile dysfunction. Bioorganic & medicinal chemistry letters 22 (23), pp. 7151-7154.
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Based on the dopamine D(4) 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(4) partial agonist (EC(50)=0.41nM). 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.
|Date:||6 October 2012|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Keywords:||Penile erection; Erectile dysfunction; Azulene; Dopamine D4; Partial agonists|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
500 Science > 570 Life sciences
600 Technology > 615 Pharmacy
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Partially|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||30 Oct 2012 14:06|
|Last Modified:||31 Oct 2012 19:52|