Počet záznamů: 1

Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents

SYSNO ASEP	0377892
Druh ASEP	J - Článek v odborném periodiku
Zařazení RIV	J - Článek v odborném periodiku
Poddruh J	Článek ve WOS
Název	Novel Bradykinin Analogues Modified in the N-Terminal Part of the Molecule with a Variety of Acyl Substituents
Tvůrce(i)	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)
Celkový počet autorů	7
Zdroj.dok.	International Journal of Peptide Research and Therapeutics - ISSN 1573-3149 Roč. 18, č. 2 (2012), s. 117-124
Poč.str.	8 s.
Jazyk dok.	eng - angličtina
Země vyd.	US - Spojené státy americké
Klíč. slova	bradykinin analogues ; B-2 receptor antagonists ; bulky acyl groups ; in vivo rat blood pressure test ; in vitro rat uterus test
Vědní obor RIV	CE - Biochemie
CEZ	AV0Z40550506 - UOCHB-X (2005-2011)
UT WOS	000303453500004
DOI	10.1007/s10989-011-9285-5
Anotace	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.
Pracoviště	Ústav organické chemie a biochemie
Kontakt	asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
Rok sběru	2013

Počet záznamů: 1