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Novel azulene derivatives for the treatment of erectile dysfunction

Löber, Stefan ; Hübner, Harald ; Buschauer, Armin ; Sanna, Fabrizio ; Argiolas, Antonio ; Melis, Maria Rosaria ; Gmeiner, Peter


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) ...


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