Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats.

@article{Lugar2004SynthesisAB,
  title={Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats.},
  author={Charles W Lugar and Michael P Clay and Terry D Lindstrom and Andrea L Woodson and David Smiley and Mark L. Heiman and Jeffrey A. Dodge},
  journal={Bioorganic & medicinal chemistry letters},
  year={2004},
  volume={14 23},
  pages={5873-6}
}
2-(2-Amino-2-methyl-propionylamino)-5-phenyl-pentanoic acid [1-[1-(4-methoxy-phenyl)-1-methyl-2-oxo-2-pyrrolidin-1-yl-ethyl]-1H-imidazol-4-yl]-amide (LY444711, 6) is an orally active ghrelin agonist that binds with high affinity to and is a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a) receptor. In rat models of feeding behavior and pharmacology, 6 creates a positive energy balance and induces adiposity by stimulating food consumption and sparing fat utilization. As… CONTINUE READING

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