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. 1995 Jul 18;92(15):7001–7005. doi: 10.1073/pnas.92.15.7001

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

A A Patchett 1, R P Nargund 1, J R Tata 1, M H Chen 1, K J Barakat 1, D B Johnston 1, K Cheng 1, W W Chan 1, B Butler 1, G Hickey 1, et al.
PMCID: PMC41459  PMID: 7624358

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.

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Selected References

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