Document Detail

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    
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.
Małgorzata Sleszyńska; Tomasz H Wierzba; Krzysztof Malinowski; Tereza Tůmová; Bernard Lammek; Jiřina Slaninová; Adam Prahl
Related Documents :
7841179 - Reversible reduction of phospholipid bound arachidonic acid after low density lipoprote...
8950509 - Ontogenesis of lipids in chick embryo retina.
1847059 - Endothelin stimulates degradation of phospholipids in isolated rat hearts.
24292109 - Bile acids increase the activity of the epithelial na(+) channel.
18502109 - Hypertriglyceridemia and hypercholesterolemia: effects of drug treatment on fatty acid ...
23395169 - Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muri...
759039 - Folic acid dependent hypersarcosinaemia.
3234339 - Immobilized ph gradients: effect of salts, added carrier ampholytes and voltage gradien...
10922489 - Lysophosphatidic acid (lpa) receptors of the edg family are differentially activated by...
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:  -    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Evaluation of nutritional quality of dried cashew nut testa using laboratory rat as a model for pigs...
Next Document:  Double-check: validation of diagnostic statistics for PLS-DA models in metabolomics studies.