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Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.

Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.

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  • 1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.

Abstract

A potent, orally active growth hormone (GH) secretagogue L-163,191 belonging to a recently synthesized structural class has been characterized. L-163,191 releases GH from rat pituitary cells in culture with EC50 = 1.3 +/- 0.09 nM and is mechanistically indistinguishable from the GH-releasing peptide GHRP-6 and the prototypical nonpeptide GH secretagogue L-692,429 but clearly distinguishable from the natural GH secretagogue, GH-releasing hormone. L-163,191 elevates GH in dogs after oral doses as low as 0.125 mg/kg and was shown to be specific in its release of GH without significant effect on plasma levels of aldosterone, luteinizing hormone, thyroxine, and prolactin after oral administration of 1 mg/kg. Only modest increases in cortisol were observed. Based on these properties, L-163,191 has been selected for clinical studies.

PMID:
7624358
[PubMed - indexed for MEDLINE]
PMCID:
PMC41459
Free PMC Article
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