Titre du document / Document title

Human galanin modulates human colonic motility in vitro : Characterization of structural requirements

Auteur(s) / Author(s)

KATSOULIS S. ; CLEMENS A. ; MORYS-WORTMANN C. ; SCHWÖRER H. ; SCHAUBE H. ; KLOMP H.-J. ; FÖLSCH U. R. ; SCHMIDT W. E. ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

Gastrointestinal Unit, Ist Dept. of Medicine, Christian-Albrecht-University of Kiel, Kiel, ALLEMAGNE

Résumé / Abstract

Background : Human galanin (hGal) is a 30-residue non-amidated gut-brain peptide that shows considerable sequence divergence compared with galanin (Gal) forms of other species. Conflicting results have been reported with regard to the structural requirements for its modulatory action on gut motility. Methods : We investigated the effect of human and rat Gal and substituted analogues of Gal on the contractility of longitudinal muscle strips of the human colon in vitro. Results : Both hGal and rGal contracted the preparations in a concentration-dependent and tetrodotoxin-resistant manner without difference in sensitivity. The NH₂-terminally truncated peptides hGal (3-30) and rGal (3-29) were inactive, whereas the NH₂-terminal fragments, hGal (1-21) and rGal (1-18), remained fully responsive. Single amino acid substitutions at NH₂-terminal positions showed divergent results : substitution of Trp² reduced significantly potency and efficacy, whereas substitutions at positions 1, 3, 4, or 5 did not markedly modify the bioactivity of Gal. Galantide, a high-affinity Gal antagonist in the central nervous system, is a full agonist in human colonic smooth muscle. Conclusion : The COOH-terminal part of Gal contributes mainly the receptor-binding affinity of the peptide, whereas the NH₂-terminal region is essential for biologic activity.

Revue / Journal Title

Scandinavian journal of gastroenterology    ISSN  0036-5521   CODEN SJGRA4 

Source / Source

1996, vol. 31, n^o5, pp. 446-451 (30 ref.)

Langue / Language

Anglais

Editeur / Publisher

Informa, Colchester, ROYAUME-UNI  (1966) (Revue)

Mots-clés anglais / English Keywords

Galanin

;

Peptides

;

Motility

;

Colon

;

In vitro

;

Biological effect

;

Animal

;

Rat

;

Rodentia

;

Mammalia

;

Vertebrata

;

Digestive system

;

Mots-clés français / French Keywords

Galanine

;

Peptide

;

Motilité

;

Côlon

;

In vitro

;

Effet biologique

;

Animal

;

Rat

;

Rodentia

;

Mammalia

;

Vertebrata

;

Appareil digestif

;

Mots-clés espagnols / Spanish Keywords

Galanina

;

Péptido

;

Motilidad

;

Colón

;

In vitro

;

Efecto biológico

;

Animal

;

Rata

;

Rodentia

;

Mammalia

;

Vertebrata

;

Aparato digestivo

;

Localisation / Location

INIST-CNRS, Cote INIST : 12513, 35400004341096.0050