title: Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents.
abstract: In the current work we present some pharmacological characteristics of ten new analogues of bradykinin (Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg) modified in the N-terminal part of the molecule with a variety of acyl substituents. Of the many acylating agents used previously with B(2) receptor antagonists, the following residues were chosen: 1-adamantaneacetic acid (Aaa), 1-adamantanecarboxylic acid (Aca), 4-tert-butylbenzoic acid (t-Bba), 4-aminobenzoic acid (Aba), 12-aminododecanoic acid (Adc), succinic acid (Sua), 4-hydroxybenzoic acid, 4-hydroxy-3-methoxybenzoic acid, 3-(4-hydroxyphenyl)propionic acid and 6-hydroxy-2-naphthoic acid. Biological activity of the compounds was assessed in the in vivo rat blood pressure test and the in vitro rat uterus test. Surprisingly, N-terminal substitution of the bradykinin peptide chain itself with aforementioned groups resulted in antagonists of bradykinin in the pressor test and suppressed agonistic potency in the uterotonic test. These interesting findings need further studies as they can be helpful for designing more potent B(2) receptor blockers.
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Sleszyńska
authors.forename: Tomasz H
authors.initials: TH
authors.lastname: Wierzba
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Malinowski
authors.forename: Tereza
authors.initials: T
authors.lastname: Tůmová
authors.forename: Bernard
authors.initials: B
authors.lastname: Lammek
authors.forename: Jiřina
authors.initials: J
authors.lastname: Slaninová
authors.forename: Adam
authors.initials: A
authors.lastname: Prahl