2. Academic Validation
  3. 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

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

  • J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h.
Iyassu K Sebhat 1,  William J Martin,  Zhixiong Ye,  Khaled Barakat,  Ralph T Mosley,  David B R Johnston,  Raman Bakshi,  Brenda Palucki,  David H Weinberg,  Tanya MacNeil,  Rubana N Kalyani,  Rui Tang,  Ralph A Stearns,  Randy R Miller,  Constantin Tamvakopoulos,  Alison M Strack,  Erin McGowan,  Doreen E Cashen,  Jennifer E Drisko,  Gary J Hom,  Andrew D Howard,  D Euan MacIntyre,  Lex H T van der Ploeg,  Arthur A Patchett,  Ravi P Nargund
Affiliations

Affiliation

  • 1 Department of Chemistry, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065-0900, USA. iyassu_sebhat@merck.com
PMID: 12361385 DOI: 10.1021/jm025539h
Abstract

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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