Document Detail


Structure-activity relationship of dermorphin on gastric secretion.
MedLine Citation:
PMID:  3569127     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The amphibian skin heptapeptide dermorphin (DM) administered intracerebroventricularly to rats significantly reduces gastric secretion. Dermorphin and 19 DM homologs and analogs were tested for their effect on gastric volume, pH, H+ ion concentration, and gastric acid output. DM, DM N-terminal pentapeptide and tetrapeptide amides, [D-Met2]DM, [Sar4]DM, [Trp5]DM, [Phe5]DM, [Gly7]DM, [Ser(Bzl)7]DM, and deamidated-DM significantly (P less than 0.01) reduced gastric acid output 2 h after injection. These data provide evidence for the following conclusions on the effect of DM on gastric secretion: ability to inhibit gastric secretion depends on the presence of the D-isomer of Ala at position 2, since [L-Ala2]DM is inactive; the shortest sequence with significant bioactivity is DM N-terminal tetrapeptide amide; the single replacement of amino acid residues in DM elicits a wide range of activities, varying from full biological activity of [Gly7]DM to those analogs with a complete lack of activity, such as [Pro4]DM and [Gly6]DM; and 4) coupling of protective groups to amino and hydroxyl groups of DM results in a significant loss of activity.
Authors:
A Guglietta; B J Irons; L H Lazarus; P Melchiorri
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Endocrinology     Volume:  120     ISSN:  0013-7227     ISO Abbreviation:  Endocrinology     Publication Date:  1987 May 
Date Detail:
Created Date:  1987-06-01     Completed Date:  1987-06-01     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  0375040     Medline TA:  Endocrinology     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  2137-43     Citation Subset:  AIM; IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Gastric Acid / secretion*
Gastric Mucosa / drug effects,  secretion
Hydrogen-Ion Concentration
Injections, Intraventricular
Kinetics
Male
Oligopeptides / administration & dosage,  pharmacology*
Opioid Peptides
Rats
Rats, Inbred Strains
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Oligopeptides; 0/Opioid Peptides; 77614-16-5/dermorphin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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