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Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.
Open accessAbstract
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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Citations
Cited by
Ghrelin: Structure and Function
Kojima, M., & Kangawa, K. (2005) · Physiological Reviews · doi:10.1152/physrev.00012.2004 · Cited by 2,810
Giustina, A., & Veldhuis, J. D. (1998) · Endocrine Reviews · doi:10.1210/edrv.19.6.0353 · Cited by 1,253
Biological, Physiological, Pathophysiological, and Pharmacological Aspects of Ghrelin
van der Lely, A. J., Tschöp, M., Heiman, M. L., & Ghigo, E. (2004) · Endocrine Reviews · doi:10.1210/er.2002-0029 · Cited by 1,187
Müller, T. D., Nogueiras, R., Andermann, M. L., Andrews, Z. B., Anker, S. D., Argente, J., Batterham, R. L., Benoit, S. C., Bowers, C. Y., Broglio, F., et al. (2015) · Molecular Metabolism · doi:10.1016/j.molmet.2015.03.005 · Cited by 1,034
Sun, Y., Wang, P., Zheng, H., & Smith, R. G. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0305930101 · Cited by 745
Metadata
- Authors
- 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.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1995-07-18
- Volume
- 92
- Issue
- 15
- Pages
- 7001-7005
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1999248363
- Cited by
- 327
- References
- 0
- FWCI
- 13.54
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. https://app.cochat.ai/papers/10.1073/pnas.92.15.7001
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- 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. https://doi.org/10.1073/pnas.92.15.7001
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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