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A non-opioid pattern characterizes inhibition of growth hormone releasing peptide binding by dynorphin-related peptides
Journal article   Peer reviewed

A non-opioid pattern characterizes inhibition of growth hormone releasing peptide binding by dynorphin-related peptides

E E Codd, V J Aloyo and R F Walker
Neuropeptides (Edinburgh), v 15(3), pp 133-137
Mar 1990
PMID: 1979153

Abstract

Animals Binding, Competitive Dynorphins - analogs & derivatives Dynorphins - pharmacology Growth Hormone-Releasing Hormone - antagonists & inhibitors Growth Hormone-Releasing Hormone - metabolism Hormones - metabolism Hypothalamus - metabolism Kinetics Male Oligopeptides - metabolism Pituitary Gland, Anterior - metabolism Protein Binding Rats Rats, Inbred Strains Structure-Activity Relationship
GHRP-6 (His-D-Trp-Ala-Trp-D-Phe-LysNH2; SK&F 110679) is a hexapeptide that specifically releases growth hormone. Although derived from methionine enkephalin, 3H-SK&F 110679 binding profiles suggest that it retains little mu or delta opioid activity. In the present study, dynorphin A was a potent inhibitor of SK&F 110679 binding. However, detailed structure-activity studies using dynorphin-related compounds suggest that the interaction between SK&F 110679 and dynorphin was non-opioid in nature. The non-opioid peptide des-Tyr-dynorphin was virtually as potent an inhibitor of 3H-SK&F 110679 binding as the intact dynorphin peptide. Additionally, the non-peptide, kappa selective ligand U-50,488 was a very weak inhibitor of 3H-SK&F 110679 binding. Since dynorphin but not U-50,488 has been reported to release growth hormone, the present results suggest that a non-opioid dynorphin site participates in SK&F 110679's growth hormone releasing action.

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Collaboration types
Industry collaboration
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Web of Science research areas
Endocrinology & Metabolism
Neurosciences
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