2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109.
Zhixiong Ye 1,  Liangqin Guo,  Khaled J Barakat,  Patrick G Pollard,  Brenda L Palucki,  Iyassu K Sebhat,  Raman K Bakshi,  Rui Tang,  Rubana N Kalyani,  Aurawan Vongs,  Airu S Chen,  Howard Y Chen,  Charles I Rosenblum,  Tanya MacNeil,  David H Weinberg,  Qianping Peng,  Constantin Tamvakopoulos,  Randy R Miller,  Ralph A Stearns,  Doreen E Cashen,  William J Martin,  Joseph M Metzger,  Alison M Strack,  D Euan MacIntyre,  Lex H T Van der Ploeg,  Arthur A Patchett,  Matthew J Wyvratt,  Ravi P Nargund
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. zhixiong_ye@merck.com
PMID: 15982875 DOI: 10.1016/j.bmcl.2005.05.109
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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