Design and Pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a Potent, Selective, Melanocortin Subtype-4 Receptor Agonist
| العنوان: | Design and Pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a Potent, Selective, Melanocortin Subtype-4 Receptor Agonist |
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| المؤلفون: | Ralph A. Stearns, Randy R. Miller, William J. Martin, Ravi P. Nargund, Erin McGowan, Lex H.T. Van der Ploeg, and Arthur A. Patchett, Andrew D. Howard, David B. R. Johnston, D. Euan MacIntyre, Rubana N. Kalyani, Khaled Barakat, Raman K. Bakshi, Ralph T. Mosley, Jennifer E. Drisko, Constantin Tamvakopoulos, Rui Tang, Alison M. Strack, Zhixiong Ye, Doreen E. Cashen, Tanya MacNeil, David H. Weinberg, Palucki Brenda, Gary J Hom, Iyassu K. Sebhat |
| المصدر: | Journal of Medicinal Chemistry. 45:4589-4593 |
| بيانات النشر: | American Chemical Society (ACS), 2002. |
| سنة النشر: | 2002 |
| مصطلحات موضوعية: | Agonist, Chemistry, medicine.drug_class, Biological activity, Pharmacology, Melanocortin receptor, THIQ, Drug Discovery, medicine, Anorectic, Molecular Medicine, Structure–activity relationship, Melanocortin, Receptor, medicine.drug |
| الوصف: | Synthetic and natural peptides that act as nonselective melanocortin receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity. |
| تدمد: | 1520-4804 0022-2623 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::039abb3a464342205d16551c756133aa https://doi.org/10.1021/jm025539h |
| رقم الأكسشن: | edsair.doi...........039abb3a464342205d16551c756133aa |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15204804 00222623 |
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