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.

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.

MeSH terms

  • Animals
  • Aza Compounds / chemical synthesis
  • Aza Compounds / pharmacology*
  • Eating / drug effects*
  • Humans
  • Male
  • Microsomes, Liver / metabolism
  • Penile Erection / drug effects*
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Piperidines / chemical synthesis
  • Piperidines / pharmacology*
  • Protein Binding
  • Quinuclidines / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Melanocortin, Type 4 / agonists*
  • Rodentia
  • Structure-Activity Relationship
  • Time Factors

Substances

  • (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)
  • Aza Compounds
  • Piperazines
  • Piperidines
  • Quinuclidines
  • Receptor, Melanocortin, Type 4