کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594381 | 981826 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel azulene derivatives for the treatment of erectile dysfunction
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel azulene derivatives for the treatment of erectile dysfunction Novel azulene derivatives for the treatment of erectile dysfunction](/preview/png/10594381.png)
چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7151-7154
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7151-7154
نویسندگان
Stefan Löber, Harald Hübner, Armin Buschauer, Fabrizio Sanna, Antonio Argiolas, Maria Rosaria Melis, Peter Gmeiner,