کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1376120 | 981951 | 2008 | 4 صفحه PDF | دانلود رایگان |
Aminomethylpiperazines, reported previously as being κ-opioid receptor agonists, were identified as lead compounds in the development of selective urotensin receptor antagonists. Optimized substitution of the piperazine moiety has provided high affinity urotensin receptor antagonists with greater than 100-fold selectivity over the κ-opioid receptor. Select compounds were found to inhibit urotensin-induced vasoconstriction in isolated rat aortic rings consistent with the hypothesis that an urotensin antagonist may be useful for the treatment of hypertension.
Aminomethylpiperazines, reported previously as being κ-opioid receptor agonists, have been developed into selective, high affinity human urotensin-II antagonists.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 16, 15 August 2008, Pages 4470–4473