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.

@article{Sebhat2002DesignAP,
  title={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.},
  author={Iyassu K Sebhat and William J Martin and Zhixiong Ye and Khaled J Barakat and Ralph T. Mosley and David B R Johnston and Raman Bakshi and Brenda Lynn Palucki and David H. Weinberg and Tanya Macneil and Rubana N Kalyani and Rui Kang Tang and Ralph A Stearns and Randy R Miller and Constantin Tamvakopoulos and Alison M. Strack and Erin McGowan and Doreen E Cashen and Jennifer E Drisko and Gary J. Hom and Andrew D. Howard and D Euan Macintyre and Lex H. T. van der Ploeg and Arthur A. Patchett and Ravi P Nargund},
  journal={Journal of medicinal chemistry},
  year={2002},
  volume={45 21},
  pages={4589-93}
}
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. 

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