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PMID: 1067621 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S.

Morphinomimetic activity of synthetic fragments of beta-lipotropin and analogs.

Ling N, Guillemin R

Abstract

In the myenteric plexus-longitudinal muscle bioassay, beta-endorphin, i.e., beta-lipotropin (beta-LPH)-[61-91], has a potency of 450 with confidence limits of 281-966 when Met5-enkephalin is used as a reference standard with a potency of 100. The primary amide and the ethylamide of Met5-enkephalin have potencies statistically overlapping with that of beta-endorphin. The primary amide of alpha-endorphin has twice the potency of the free acid form of alpha-endorphin. An intact NH2-terminal tyrosine is not necessary for full intrinsic activity. The shortest fragment of beta-LPH with morphinomimetic activity is beta-LPH-[61-64].

MeSH Terms
Amino Acid Sequence Animals Biological Assay Guinea Pigs Oligopeptides/pharmacology Peptide Fragments/pharmacology Structure-Activity Relationship beta-Lipotropin/pharmacology
Chemicals
Oligopeptides Peptide Fragments beta-Lipotropin
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Ling N
Guillemin R
References (16)
16 references, click to expand
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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
Published
1976-09-00
Pages
3308-10
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC431021
Subset
IM
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