Bradykinin B1 receptors in human umbilical vein.
The present study was undertaken to demonstrate the presence of bradykinin B1 receptors mediating contraction of human umbilical vein. The bradykinin B1 receptor selective agonist, des-Arg9-bradykinin, produced a dose-dependent contractile response of human umbilical vein rings. Furthermore, des-Arga-bradykinin-mediated response increased in a time-dependent manner in vitro. The maximal response to des-Arg9-bradykinin, expressed as percentage of the maximum elicited by serotonin, was: 10 +/- 2 at 15 min, 55 +/- 5 at 120 min and 80 +/- 3 at 300 min. Des-Arg9-bradykinin-mediated contractions were inhibited by the specific bradykinin B1 receptor antagonist des-Arg9-[Leu8]bradykinin which produced parallel shifts in the dose-response curve to the selective bradykinin B1 receptor agonist. Schild regression analysis of data established a pA2 value of 6.16 +/- 0.06. Kinin-induced contraction was not modified by pre-treatment with indomethacin (10 microM), a cyclo-oxygenase inhibitor. On the other hand, continuous exposure to the anti-inflammatory steroid dexamethasone (100 microM) or to the protein synthesis inhibitor cycloheximide (70 microM) largely prevented the sensitization to des-Arg9-bradykinin in incubated human umbilical vein rings. These results confirm the presence of bradykinin B1 receptors which mediate contraction in isolated human umbilical vein. These responses are up-regulated in a time- and protein synthesis-dependent process.
Sardi
S P
SP
Departamento de Farmacología, Facultad de Medicina, Universidad de Buenos Aires, Argentina.
Pérez
H
H
Antúnez
P
P
Rothlin
R P
RP
D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D001920:Bradykinin / Q000031:analogs & derivatives / Q000494:pharmacology; D065168:Bradykinin Receptor Antagonists; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000502:physiology; D011247:Pregnancy; D043783:Receptor, Bradykinin B1; D018002:Receptors, Bradykinin / Q000819:agonists / Q000187:drug effects*; D014471:Umbilical Veins / Q000187:drug effects*; D015854:Up-Regulation / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D065168:Bradykinin Receptor Antagonists; D016861:Cyclooxygenase Inhibitors; D043783:Receptor, Bradykinin B1; D018002:Receptors, Bradykinin; C024626:bradykinin, des-Arg(9)-; C051090:bradykinin, Leu(8)-des-Arg(9)-; C065679:icatibant; D003907:Dexamethasone; D001920:Bradykinin