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  • Title: Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats.
    Author: Lugar CW, Clay MP, Lindstrom TD, Woodson AL, Smiley D, Heiman ML, Dodge JA.
    Journal: Bioorg Med Chem Lett; 2004 Dec 06; 14(23):5873-6. PubMed ID: 15501059.
    Abstract:
    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 an orally active ghrelin agonist, 6 represents a new pharmacological tool to investigate the orexigenic role of ghrelin in regulating energy homeostasis.
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