DOI: 10.1073/pnas.92.15.7001. Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.

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

10.1073/pnas.92.15.7001

Crossref journal-article

Proceedings of the National Academy of Sciences

Proceedings of the National Academy of Sciences (341)

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.

Bibliography

Patchett, A. A., Nargund, R. P., Tata, J. R., Chen, M. H., Barakat, K. J., Johnston, D. B., Cheng, K., Chan, W. W., Butler, B., & Hickey, G. (1995). Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proceedings of the National Academy of Sciences, 92(15), 7001â7005.

Authors 10

A A Patchett (first)
R P Nargund (additional)
J R Tata (additional)
M H Chen (additional)
K J Barakat (additional)
D B Johnston (additional)
K Cheng (additional)
W W Chan (additional)
B Butler (additional)
G Hickey (additional)

References 0 Referenced 263

None

Dates

Type	When
Created	19 years, 3 months ago (May 31, 2006, 9:16 a.m.)
Deposited	3 years, 4 months ago (April 13, 2022, 1:51 p.m.)
Indexed	4 days, 1 hour ago (Sept. 3, 2025, 6:22 a.m.)
Issued	30 years, 1 month ago (July 18, 1995)
Published	30 years, 1 month ago (July 18, 1995)
Published Online	30 years, 1 month ago (July 18, 1995)
Published Print	30 years, 1 month ago (July 18, 1995)

Funders 0

None

BibTeX

@article{Patchett_1995, title={Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.}, volume={92}, ISSN={1091-6490}, url={http://dx.doi.org/10.1073/pnas.92.15.7001}, DOI={10.1073/pnas.92.15.7001}, number={15}, journal={Proceedings of the National Academy of Sciences}, publisher={Proceedings of the National Academy of Sciences}, author={Patchett, A A and Nargund, R P and Tata, J R and Chen, M H and Barakat, K J and Johnston, D B and Cheng, K and Chan, W W and Butler, B and Hickey, G}, year={1995}, month=jul, pages={7001–7005} }

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