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Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents
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SYSNO ASEP 0377892 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents Author(s) Sleszynska, M. (PL)
Wierzba, T. H. (PL)
Malinowski, K. (PL)
Tůmová, Tereza (UOCHB-X) RID
Lammek, B. (PL)
Slaninová, Jiřina (UOCHB-X)
Prahl, A. (PL)Number of authors 7 Source Title International Journal of Peptide Research and Therapeutics - ISSN 1573-3149
Roč. 18, č. 2 (2012), s. 117-124Number of pages 8 s. Language eng - English Country US - United States Keywords bradykinin analogues ; B-2 receptor antagonists ; bulky acyl groups ; in vivo rat blood pressure test ; in vitro rat uterus test Subject RIV CE - Biochemistry CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000303453500004 DOI 10.1007/s10989-011-9285-5 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2013
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