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PMID: 6118865 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

Specific receptor for the opioid peptide dynorphin: structure--activity relationships.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 78 ·No. 10 ·1981-10-00 ·Pages 6543-7

Chavkin C, Goldstein A

Abstract

The structural features responsible for the high potency and opiate receptor specificity of the opioid peptide dynorphin in the guinea pig ileum myenteric plexus were examined. Successive removal of COOH-terminal amino acids from dynorphin-(1--13) demonstrated important contributions of lysine-13, lysine-11, and arginine-7 to the potency. Removal of the NH2-terminal tyrosine abolished the biologic activity. Several other structural modifications were shown to affect potency: substitution of D-alanine for glycine-2 reduced the potencies of dynorphin-(1--13) amide, -(1--11), and -(1--10); and methyl esterification of the COOH terminus enhanced the potencies of dynorphin-(1--12), -(1--10), -(1--9), -(1--8), and -(1--7). Within the dynorphin sequence, lysine-11 and arginine-7 were found to be important for selectivity of interaction with the dynorphin receptor, which is distinguishable from the mu receptor in this tissue.

MeSH Terms
Animals Biological Assay Dynorphins Endorphins/metabolism,pharmacology Guinea Pigs Ileum/drug effects Myenteric Plexus/drug effects Receptors, Opioid/metabolism Structure-Activity Relationship
Chemicals
Endorphins Receptors, Opioid dynorphin receptor Dynorphins
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Chavkin C
Goldstein A
References (20)
20 references, click to expand
  1. Morphine-tolerant longitudinal muscle strip from guinea-pig ileum.
    Br J Pharmacol. 1973 Aug;48(4):655-66 PMID: 4799172
  2. Opiate activity and receptor selectivity of dynorphin1-13 and related peptides.
    Neurosci Lett. 1980 Oct 20;20(1):79-83 PMID: 6133254
  3. A synthetic peptide with morphine-like pharmacologic action.
    Life Sci. 1975 Dec 1;17(11):1643-54 PMID: 1207378
  4. Morphinomimetic activity of synthetic fragments of beta-lipotropin and analogs.
    Proc Natl Acad Sci U S A. 1976 Sep;73(9):3308-10 PMID: 1067621
  5. (D-Ala2)-Met-enkephalinamide: a potent, long-lasting synthetic pentapeptide analgesic.
    Science. 1976 Oct 15;194(4262):330-2 PMID: 968485
  6. Structure-activity relationships of methionine-enkephalin.
    J Pharm Pharmacol. 1976 Aug;28(8):660-1 PMID: 11324
  7. Endogenous opioid peptides: multiple agonists and receptors.
    Nature. 1977 Jun 9;267(5611):495-9 PMID: 195217
  8. ACTH: a short introductory review.
    Ann N Y Acad Sci. 1977 Oct 28;297:3-26 PMID: 211904
  9. Biosynthesis of bacterial glycogen. Isolation and characterization of the pyridoxal-P allosteric activator site and the ADP-glucose-protected pyridoxal-P binding site of Escherichia coli B ADP-glucose synthase.
    J Biol Chem. 1978 Nov 10;253(21):7638-45 PMID: 359552
  10. alpha-Neo-endorphin : a "big" Leu-enkephalin with potent opiate activity from porcine hypothalami.
    Biochem Biophys Res Commun. 1979 Jan 15;86(1):153-60 PMID: 435296
  11. Purification and properties of a prolyl endopeptidase from rabbit brain.
    J Neurochem. 1979 Aug;33(2):461-9 PMID: 469536
  12. Phosphorylation-dephosphorylation of enzymes.
    Annu Rev Biochem. 1979;48:923-59 PMID: 38740
  13. Dynorphin-(1-13), an extraordinarily potent opioid peptide.
    Proc Natl Acad Sci U S A. 1979 Dec;76(12):6666-70 PMID: 230519
  14. Highly specific opiate receptors for dynorphin-(1-13) in the mouse vas deferens.
    Eur J Pharmacol. 1980 Mar 21;62(2-3):235-6 PMID: 6103811
  15. Structure-activity relationships of enkephalin-like peptides.
    Annu Rev Pharmacol Toxicol. 1980;20:81-110 PMID: 6247963
  16. A specific radioimmunoassay for the novel opioid peptide dynorphin.
    Life Sci. 1980 Jul 7;27(1):75-86 PMID: 6105608
  17. Behavioral effects and in vivo degradation of intraventricularly administered dynorphin-(1-13) and D-Ala2-dynorphin-(1-11) in rats.
    Life Sci. 1980 Sep 8;27(10):883-92 PMID: 7191035
  18. Formation of biologically active peptides.
    Proc R Soc Lond B Biol Sci. 1980 Oct 29;210(1178):45-59 PMID: 6107930
  19. Demonstration of a specific dynorphin receptor in guinea pig ileum myenteric plexus.
    Nature. 1981 Jun 18;291(5816):591-3 PMID: 6264311
  20. Effect of morphine on adrenergic transmission in the mouse vas deferens. Assessment of agonist and antogonist potencies of narcotic analgesics.
    Br J Pharmacol. 1975 Mar;53(3):371-81 PMID: 236796
Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.78.10.6543
Published
1981-10-00
Pages
6543-7
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC349077
Subset
IM
Grants
NIDA NIH HHS · DA-1199 · United States
NIDA NIH HHS · DA-7063 · United States
External Links
PubMed source DOI: 10.1073/pnas.78.10.6543 PMC Full Text View journal details
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