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

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

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

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Tata, J. R. Chen, M. H. Chan, W. W. Nargund, R. P. Hickey, G. Johnston, D. B. Butler, B. Cheng, K. Barakat, K. J. Patchett, A. A.
Description	Author Affiliation: Patchett AA ( Department 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.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	15
Volume Number	92
Language	English
Publisher	National Academy of Sciences
Publisher Date	1995-08-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Growth Hormone Secretion Indoles Administration & Dosage Pituitary Gland Drug Effects Spiro Compounds Administration, Oral Aldosterone Blood Amino Acid Sequence Animals Benzazepines Pharmacology Cells, Cultured Drug Design Drug Synergism Injections, Intravenous Luteinizing Hormone Molecular Sequence Data Oligopeptides Prolactin Structure-Activity Relationship Tetrazoles Thyroxine Comparative Study Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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