title: Structure-activity studies of bradykinin analogues on rat mast cell histamine release.
abstract: Bradykinin (BK), kallidin (KD), and various analogues induced histamine release from rat mast cells. The results obtained with substituted analogues of BK indicated that: 1) the presence of both Arg residues at position 1 and 9 of kinins was favorable to confer histamine-releasing activity, 2) acetylation of the N-terminal amino acid residue led to a drastic reduction of this activity, 3) addition of a D-Arg residue at the N-terminus reduced their activity, as well as trans-4-hydroxyproline (Hyp) substitutions at position 2 or 3,4) D-Arg0 addition and Hyp3 substitution were synergistic in lowering activity, and 5) D-Phe7 substitution led to enhanced histamine-releasing activity.
authors.affiliation: Centre de Recherche Public-Santé, Neuroimmunologie and Inflammation, Luxembourg, France.
authors.forename: J L
authors.initials: JL
authors.lastname: Bueb
authors.forename: M
authors.initials: M
authors.lastname: Mousli
authors.forename: Y
authors.initials: Y
authors.lastname: Landry
authors.forename: D
authors.initials: D
authors.lastname: Regoli
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D008297:Male; D008407:Mast Cells / Q000187:drug effects* / Q000378:metabolism; D008969:Molecular Sequence Data; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D001920:Bradykinin