Role of N-terminal active sites of galanin in neurally evoked circular muscle contractions in the guinea-pig ileum. 1997

H Kakuyama, and A Kuwahara, and T Mochizuki, and M Hoshino, and N Yanaihara
Laboratory of Bioorganic Chemistry, School of Pharmaceutical Sciences, University of Shizuoka, Yada, Japan.

Synthetic galanin-related peptides and several galanin-(1-15)ol analogs were used to examine structure-function relationships of the N-terminal active site of galanin in more detail, using the guinea-pig ileum. The synthetic peptides examined showed their inhibitory activity on the neurally evoked circular muscle contractions with the following order of potency: rat, human and tuna galanin, galanin-(1-15)ol and [D-Trp8]galanin-(1-15)ol > N alpha-acetylated galanin-(2-15)ol, [Ala6,D-Trp8]galanin-(1-15)ol, galanin-(1-15) > tuna galanin-(1-15), [D-Ala8]galanin-(1-15)ol, N alpha-acetylated galanin-(1-15)ol. In contrast, [D-Thr6]galanin-(1-15)ol, [D-Tyr9]galanin-(1-15)ol and [D-Trp9]galanin-(1-15)ol were ineffective and showed no antagonistic activities to galanin. These results suggest that the L-configuration at positions 6 and 9 seems to be important for the inhibitory action of galanin on the neurally evoked guinea-pig circular muscle contractions.

UI MeSH Term Description Entries
D007082 Ileum The distal and narrowest portion of the SMALL INTESTINE, between the JEJUNUM and the ILEOCECAL VALVE of the LARGE INTESTINE.
D008969 Molecular Sequence Data Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories. Sequence Data, Molecular,Molecular Sequencing Data,Data, Molecular Sequence,Data, Molecular Sequencing,Sequencing Data, Molecular
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D004558 Electric Stimulation Use of electric potential or currents to elicit biological responses. Stimulation, Electric,Electrical Stimulation,Electric Stimulations,Electrical Stimulations,Stimulation, Electrical,Stimulations, Electric,Stimulations, Electrical
D005769 Gastrointestinal Motility The motor activity of the GASTROINTESTINAL TRACT. Intestinal Motility,Gastrointestinal Motilities,Intestinal Motilities,Motilities, Gastrointestinal,Motilities, Intestinal,Motility, Gastrointestinal,Motility, Intestinal
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000595 Amino Acid Sequence The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION. Protein Structure, Primary,Amino Acid Sequences,Sequence, Amino Acid,Sequences, Amino Acid,Primary Protein Structure,Primary Protein Structures,Protein Structures, Primary,Structure, Primary Protein,Structures, Primary Protein
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining

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