Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Griesbacher, T; Lembeck, F.
Analysis of the antagonistic actions of HOE 140 and other novel bradykinin analogues on the guinea-pig ileum.
Eur J Pharmacol. 1992; 211(3):393-398
Doi: 10.1016%2F0014-2999%2892%2990397-M
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- Führende Autor*innen der Med Uni Graz
- Griesbacher Thomas
- Co-Autor*innen der Med Uni Graz
- Lembeck Fred
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- Abstract:
- The type of antagonism exhibited by three novel bradykinin (BK) antagonists, D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]BK (HOE 140, compound I), D-Arg-[Hyp3,D-Tic7,Oic8]BK (compound II) and [Arg(Tos)1,Hyp3,Thi5,D-Tic7,Oic8]BK (compound III), was compared with that of a conventional antagonist, D-Arg-[Hyp2,Thi5,8,D-Phe7]BK (compound IV), on the guinea-pig ileum. The novel compounds induced rightward displacements of cumulative concentration-response curves to BK, accompanied by a progressive reduction of the maximum effect (Emax) without a significant decrease in the slope, whereas no reduction of Emax was observed with compound IV. Actions of substance P on the guinea-pig ileum and of vasopressin on the rat uterus remained completely unaffected. It is concluded that as the novel BK analogues show competitive as well as non-competitive inhibition in the guinea-pig ileum, but the inhibition is reversible and specific, they are dual antagonists.
- Find related publications in this database (using NLM MeSH Indexing)
- Amino Acid Sequence -
- Animals -
- Binding, Competitive -
- Bradykinin - analogs and derivatives
- Guinea Pigs - analogs and derivatives
- Ileum - drug effects
- Kinetics - drug effects
- Molecular Sequence Data - drug effects
- Muscle, Smooth - drug effects
- Oligopeptides - pharmacology
- Find related publications in this database (Keywords)
- Bradykinin Receptor Antagonists
- Smooth Muscle