کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379610 | 982032 | 2005 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The melanocortin-4 receptor (MC4R) plays an important role in the regulation of energy homeostasis. Recent studies have shown that blockade of the MC4R reverses tumor-induced weight loss in mice. Herein, we describe the synthesis and identification of potent and selective non-peptide antagonists of the human MC4R from a series of 2-ethoxycarbonylcyclohexyl-piperazines. Compound 12i was found to possess low nanomolar affinity for the MC4R, and exhibit oral bioavailability in rats. More importantly, when administered orally to mice (10 mg/kg), it led to statistically significant increases in food intake over a 24-h period.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 19, 1 October 2005, Pages 4389–4395
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 19, 1 October 2005, Pages 4389–4395
نویسندگان
Fabio C. Tucci, Nicole S. White, Stacy Markison, Margaret Joppa, Joe A. Tran, Beth A. Fleck, Ajay Madan, Brian P. Dyck, Jessica Parker, Joseph Pontillo, L. Melissa Arellano, Dragan Marinkovic, Wanlong Jiang, Caroline W. Chen, Kathleen R. Gogas,