Loeber, Stefan and Huebner, 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. ISSN 0960-894X,
Full text not available from this repository. (Request a copy)Abstract
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 alpha-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 (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. (C) 2012 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DOPAMINE-D4 RECEPTOR LIGANDS; INDUCE PENILE ERECTION; BINDING EXPERIMENTS; HIGH-AFFINITY; CELL-LINE; MALE RATS; APOMORPHINE; EFFICACY; AGONISTS; PHARMACOLOGY; Penile erection; Erectile dysfunction; Azulene; Dopamine D-4; Partial agonists |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 04 May 2020 05:47 |
| Last Modified: | 04 May 2020 05:47 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17714 |
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