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