Document Detail

Structure-activity relationship of dermorphin on gastric secretion.
MedLine Citation:
PMID:  3569127     Owner:  NLM     Status:  MEDLINE    
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.
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
Gastric Acid / secretion*
Gastric Mucosa / drug effects,  secretion
Hydrogen-Ion Concentration
Injections, Intraventricular
Oligopeptides / administration & dosage,  pharmacology*
Opioid Peptides
Rats, Inbred Strains
Structure-Activity Relationship
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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