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 |
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| Authors: | Ye Zhixiong Guo Liangqin Barakat Khaled J Pollard Patrick G Palucki Brenda L Sebhat Iyassu K Bakshi Raman K Tang Rui Kalyani Rubana N Vongs Aurawan Chen Airu S Chen Howard Y Rosenblum Charles I MacNeil Tanya Weinberg David H Peng Qianping Tamvakopoulos Constantin Miller Randy R Stearns Ralph A Cashen Doreen E Martin William J Metzger Joseph M Strack Alison M MacIntyre D Euan Van der Ploeg Lex H T Patchett Arthur A Wyvratt Matthew J Nargund Ravi P |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. zhixiong_ye@merck.com |
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| Abstract: | 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. |
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