New acylated bradykinin analogues: effect on rat blood pressure and rat uterus

2005 ◽  
Vol 11 (7) ◽  
pp. 436-439 ◽  
Author(s):  
Olga Dawidowska ◽  
Adam Prahl ◽  
Tomasz Wierzba ◽  
Łukasz Nowakowski ◽  
Wioleta Kowalczyk ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Rat Uterus ◽  
Rat Blood ◽  
Bradykinin Analogues

scholarly journals New bradykinin analogues acylated on the N-terminus: effect on rat uterus and blood pressure.

2007 ◽  
Vol 54 (1) ◽  
pp. 193-198 ◽  
Author(s):  
Olga Labudda ◽  
Tomasz Wierzba ◽  
Dariusz Sobolewski ◽  
Małgorzata Sleszyńska ◽  
Łukasz Gawiński ◽  
...  
Keyword(s):  
Blood Pressure ◽  
The Other ◽  
Rat Uterus ◽  
Rat Blood ◽  
Other Hand ◽  
N Terminus ◽  
Pressure Lowering ◽  
Bradykinin Analogues ◽  
Group D

Our previous studies suggested that acylation of the N-terminus of several known B2 antagonists with various kinds of bulky acyl groups consistently improved their antagonistic potency in rat blood pressure assay. On the other hand, our earlier observations also seemed to suggest that the effects of acylation on the contractility of isolated rat uterus depended substantially on the chemical character of the acyl group, as we observed that this modification might either change the range of antagonism or even transform it into agonism. Bearing all this in mind, we decided to synthesize seven new analogues of bradykinin by N-terminal acylation with various acyl groups of a moderately potent B2 antagonist, previously synthesized by Stewart's group, D-Arg-Arg-Pro-Hyp-Gly-Thr-Ser-D-Phe-Thi-Arg. The analogues were tested in vitro for their blood pressure-lowering and uterotonic activities. The modifications either preserved or increased the antagonistic potency in the rat blood pressure test. On the other hand, all seven substituents negatively influenced the interaction with the rat uterine receptors. Our results may be helpful for designing new B2 agonists and antagonists.

Studies with Endothelin-3 and Endothelin-1 on Rat Blood Pressure and Isolated Tissues

1989 ◽  
Vol 13 ◽  
pp. S191-192 ◽  
Author(s):  
Rachel A. Spokes ◽  
Mohammad A. Ghatei ◽  
Stephen R. Bloom
Keyword(s):  
Blood Pressure ◽  
Rat Blood ◽  
Endothelin 1 ◽  
Endothelin 3 ◽  
Isolated Tissues

Rat blood pressure during ethanol withdrawal

Alcohol ◽  
1984 ◽  
Vol 1 (4) ◽  
pp. 315-318
Author(s):  
Leonard Y. Koda ◽  
Samuel G. Madamba ◽  
Floyd E. Bloom
Keyword(s):  
Blood Pressure ◽  
Ethanol Withdrawal ◽  
Rat Blood

scholarly journals Possible mechanisms of the triphasic effects of neurotensin on the rat blood pressure.

1981 ◽  
Vol 31 (6) ◽  
pp. 1043-1049 ◽  
Author(s):  
Mariko OISHI ◽  
Chiyoko INAGAKI ◽  
Motokazu FUJIWARA ◽  
Shuji TAKAORI ◽  
Haruaki YAJIMA ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Rat Blood

scholarly journals New bradykinin B(2) receptor antagonists - influence of C-terminal segment modifications on their pharmacological properties.

2009 ◽  
Vol 56 (4) ◽  
Author(s):  
Małgorzata Sleszyńska ◽  
Anna Kwiatkowska ◽  
Dariusz Sobolewski ◽  
Tomasz H Wierzba ◽  
Joanna Katarzyńska ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Terminal Segment ◽  
Pharmacological Properties ◽  
Rat Uterus ◽  
New Information ◽  
Pressure Tests ◽  
Pressure Test ◽  
Receptor Blockers ◽  
Beta 2 ◽  
Relationship Of

In the present study we describe the synthesis and some pharmacological properties of eight new analogues of bradykinin (BK). Two peptides were designed by substitution of position 7 or 8 of the known [D-Arg(0),Hyp(3),Thi(5,8),D-Phe(7)]BK antagonist (Stewart's antagonist) with L-pipecolic acid (L-Pip). The next two analogues were obtained by replacement of the d-Phe residue in position 7 of the Stewart's peptide with L-beta(2)-isoproline (L-beta(2)-iPro) or L-beta(3)-homoproline (L-beta(3)-hPro). The four analogues mentioned above were also prepared in N-acylated form with 1-adamantaneacetic acid (Aaa). Biological activity of the compounds was assessed by isolated rat uterus and rat blood pressure tests. Our results showed that L-Pip in position 7 slightly increased antagonistic potency in the blood pressure test, but it turned the analogue into an agonist in the rat uterus test. Replacement of Thi by L-Pip in position 8 also enhanced antagonism in the rat pressure test but preserved the antagonism in the rat uterus test. L-beta(2)-iPro or L-beta(3)-hPro in position 7 decreased the potencies in both tests. We also demonstrated that acylation of the N-terminus did not increase, as was claimed previously, the antagonistic potencies of the resulting peptides. The results thus support the hypothesis about the existence of different types of BK receptors in the rat uterus and blood vessels. Our studies provide new information about the structure-activity relationship of BK antagonists which may help in designing more potent BK receptor blockers.

scholarly journals The Effects of a Chactoid Scorpion Venom and Its Purified Toxins on Rat Blood Pressure and Mast Cells Histamine Release

Toxins ◽  
2013 ◽  
Vol 5 (8) ◽  
pp. 1332-1342 ◽  
Author(s):  
Keren Ettinger ◽  
Gadi Cohen ◽  
Tatjana Momic ◽  
Philip Lazarovici
Keyword(s):  
Blood Pressure ◽  
Mast Cells ◽  
Histamine Release ◽  
Scorpion Venom ◽  
Rat Blood

scholarly journals POSSIBLE MECHANISMS OF THE TRIPHASIC EFFECTS OF NEUROTENSIN ON THE RAT BLOOD PRESSURE

1981 ◽  
Vol 31 (6) ◽  
pp. 1043-1050
Author(s):  
Mariko OISHI ◽  
Chiyoko INAGAKI ◽  
Motokazu FUJIWARA ◽  
Shuji TAKAORI ◽  
Haruaki YAJIMA ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Rat Blood
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