Počet záznamů: 1

Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule

  1. 1.
    0360968 - UOCHB-X 2012 RIV GB eng J - Článek v odborném periodiku
    Sleszynska, M. - Wierzba, T. H. - Malinowski, K. - Borovičková, Lenka - Maluch, I. - Sobolewski, D. - Lammek, B. - Slaninová, Jiřina - Prahl, A.
    Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule.
    Journal of Peptide Science. Roč. 17, č. 5 (2011), s. 366-372 ISSN 1075-2617
    Výzkumný záměr: CEZ:AV0Z40550506
    Klíčová slova: bradykinin analogues * B2 receptor antagonists * sterically restricted residue * in vivo rat blood pressure test * in vitro rat uterus
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 1.799, rok: 2011

    Achiral non-coded amino acids (N-benzylglycine, 2-aminomethylphenylacetic acid or 3-aminophenylacetic acid) were substituted at position 7 of the B-2 receptor antagonist [D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK. The N-terminal amino group of the analogues was either free or acylated with 1-Aca or Aaa. Biological activity of the compounds was assessed in the in vitro rat uterus test and the in vivo rat blood pressure test. Substitution in position 7 resulted in a decrease in antagonistic potency or change of the activity into agonistic one. Acylation of the N-terminus enhanced antagonistic properties of the resulting peptides in the rat blood pressure test.
    Trvalý link: http://hdl.handle.net/11104/0198399