| Titolo: | Novel azulene drivative for the treatment of erectile dysfunction |
| Autori: | Löber S
Hübner H
Buschauer A
Gmeiner P. |
| Data di pubblicazione: | 2012 |
| Rivista: | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
| Citazione: | Novel azulene drivative for the treatment of erectile dysfunction / Löber S; Hübner H; Buschauer A; Sanna F; Argiolas A; Melis MR; Gmeiner P. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 22:23(2012), pp. 7151-7154. |
| 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
a-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. |
| Handle: | http://hdl.handle.net/11584/103687 |
| Tipologia: | 1.1 Articolo in rivista
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