Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist

التفاصيل البيبلوغرافية
العنوان: Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist
المؤلفون: Doreen E. Cashen, Constantin Tamvakopoulos, Qianping Peng, William J. Martin, David H. Weinberg, Charles Rosenblum, Arthur A. Patchett, Tanya MacNeil, Patrick G. Pollard, Zhixiong Ye, Raman K. Bakshi, Ralph A. Stearns, Rubana N. Kalyani, Palucki Brenda, Joseph M. Metzger, Alison M. Strack, Lex H.T. Van der Ploeg, D. Euan MacIntyre, Iyassu K. Sebhat, Aurawan Vongs, Airu S. Chen, Ravi P. Nargund, Liangqin Guo, Matthew J. Wyvratt, Randy R. Miller, Rui Tang, Howard Y. Chen, Khaled J. Barakat
المصدر: Bioorganic & Medicinal Chemistry Letters. 15:3501-3505
بيانات النشر: Elsevier BV, 2005.
سنة النشر: 2005
مصطلحات موضوعية: Male, Agonist, Quinuclidines, Time Factors, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Rodentia, Carboxamide, Biochemistry, Chemical synthesis, Piperazines, Rats, Sprague-Dawley, Eating, Structure-Activity Relationship, Piperidines, In vivo, Drug Discovery, medicine, Animals, Humans, Receptor, Molecular Biology, Aza Compounds, Bicyclic molecule, Chemistry, Penile Erection, digestive, oral, and skin physiology, Organic Chemistry, Small molecule, Rats, Microsomes, Liver, Receptor, Melanocortin, Type 4, Molecular Medicine, Melanocortin, Protein Binding
الوصف: A novel isoquinuclidine containing selective melanocortin subtype-4 receptor small molecule agonist, 3 (RY764), is reported. Its in vivo characterization revealed mechanism-based food intake reduction and erectile activity augmentation in rodents.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eec96b03aa1e5f2ba3d3c429b0a51544
https://doi.org/10.1016/j.bmcl.2005.05.109
حقوق: CLOSED
رقم الأكسشن: edsair.doi.dedup.....eec96b03aa1e5f2ba3d3c429b0a51544
قاعدة البيانات: OpenAIRE