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1.
Eur J Pharmacol ; 342(2-3): 359-66, 1998 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-9548409

RESUMO

The bradykinin-induced rise in intracellular Ca2+ concentration ([Ca2+]i) and the bradykinin receptor involved in this response were characterized in bovine pulmonary artery endothelial cells. It was found that bradykinin induces an intracellular biphasic Ca2+ response, consisting of a transient peak followed by an elevated plateau phase. Both bradykinin and the bradykinin B1 receptor agonist, des-Arg9-bradykinin, induced a concentration-dependent increase in [Ca2+]i, but the bradykinin-induced rise was much greater. Moreover, the bradykinin-induced [Ca2+]i rise could be inhibited by the bradykinin B2 receptor antagonists, D-Arg0[Hyp3, Thi(5,8), D-Phe7]bradykinin and Hoe 140 (D-Arg[Hyp3, Thi5, D-Tic7, Oic8]bradykinin), but not by the bradykinin B1 receptor antagonist, des-Arg9-[Leu8]bradykinin. From these results it can be concluded that a bradykinin B2 receptor is involved in this response. Furthermore, we found that the tachykinin NK1 receptor antagonist, RP67580 ([imino 1 (methoxy-2-phenyl)-2 ethyl]-2 diphenyl 7,7 perhydroisoindolone-4 (3aR, 7aR)), and its negative enantiomer, RP68651 (2-[1-imino 2-(2 methoxy phenyl) ethyl] 7,7 diphenyl 4-perhydroisoindolone (3aS-7aS)), could inhibit the bradykinin-induced [Ca2+]i response, although no functional tachykinin NK1 receptors were found. Binding studies evidenced no binding of RP67580 or RP68651 to the bradykinin receptor. We conclude that RP67580 inhibits the bradykinin-induced rise in [Ca2+]i via a bradykinin B2 receptor-independent mechanism.


Assuntos
Bradicinina/antagonistas & inibidores , Cálcio/metabolismo , Endotélio Vascular/metabolismo , Indóis/farmacologia , Músculo Liso Vascular/metabolismo , Antagonistas dos Receptores de Neurocinina-1 , Artéria Pulmonar/metabolismo , Animais , Bradicinina/farmacologia , Bovinos , Células Cultivadas , Endotélio Vascular/efeitos dos fármacos , Corantes Fluorescentes , Fura-2 , Isoindóis , Músculo Liso Vascular/efeitos dos fármacos , Artéria Pulmonar/efeitos dos fármacos
2.
Naunyn Schmiedebergs Arch Pharmacol ; 356(1): 134-8, 1997 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-9228200

RESUMO

In the present study, the effect of bradykinin on basal and precontracted mouse-isolated trachea was investigated. In basal conditions mouse-isolated tracheal rings do not respond to bradykinin. However, when the tracheal rings were precontracted with carbachol (10(-7) M) a relaxation with bradykinin (3 x 10(-9)-3 x 10(-7)) was found. The maximal response amounted 69.7+/-4.1% (n=15) with a pD2 value of 7.2+/-0.21. The selective bradykinin B2 receptor antagonist HOE 140 (10(-10)-10(-8) M) antagonized the bradykinin-induced relaxation, while the bradykinin B1 receptor antagonist des-Arg9-Leu8-bradykinin (10(-6) M) had no influence. The selective bradykinin B1 receptor agonist des-Arg9-bradykinin (10(-6) M) caused a small relaxation (8.4+/-2.5%, n=6), which could be antagonized completely by the selective bradykinin B1 receptor antagonist des-Arg9-Leu8-bradykinin (10(-6) M) while addition of the selective bradykinin B2 receptor antagonist HOE 140 (10(-8) M) was without effect. In the presence of indomethacin (10(-6) M) the relaxation of bradykinin was completely abolished. Pretreatment of the tracheal rings with capsaicin, or the presence of the selective NK1 receptor antagonist RP 67851 (10(-6) M) or the presence of the nitric oxide synthase inhibitor L-NAME (3 x 10(-4) M) had no effect on the bradykinin-induced relaxation. In conclusion, these results demonstrate that the mouse-isolated tracheal is a preparation in which bradykinin exerts a relaxant response via stimulation of bradykinin B2 receptors. This response is probably mediated by prostaglandins.


Assuntos
Bradicinina/farmacologia , Contração Muscular/efeitos dos fármacos , Traqueia/efeitos dos fármacos , Animais , Bradicinina/antagonistas & inibidores , Antagonistas dos Receptores da Bradicinina , Capsaicina/farmacologia , Técnicas In Vitro , Indóis/farmacologia , Indometacina/farmacologia , Isoindóis , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Músculo Liso/efeitos dos fármacos , NG-Nitroarginina Metil Éster/farmacologia , Receptores da Bradicinina/agonistas , Receptores da Bradicinina/efeitos dos fármacos
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