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Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents.
MedLine Citation:
PMID:  22593719     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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:
Małgorzata Sleszyńska; Tomasz H Wierzba; Krzysztof Malinowski; Tereza Tůmová; Bernard Lammek; Jiřina Slaninová; Adam Prahl
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-1-3
Journal Detail:
Title:  International journal of peptide research and therapeutics     Volume:  18     ISSN:  1573-3904     ISO Abbreviation:  -     Publication Date:  2012 Jun 
Date Detail:
Created Date:  2012-5-17     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101252761     Medline TA:  Int J Pept Res Ther     Country:  -    
Other Details:
Languages:  ENG     Pagination:  117-124     Citation Subset:  -    
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