Iloprost and cicaprost (IP-receptor agonists) induced relaxations in the histamine- (50 μM) contracted human bronchial preparations (pD2 values, 6.63±0.12 and 6.86±0.08; Emax values, 90±04 and 65±08% of the papaverine response for iloprost (n=6) and cicaprost (n=3), respectively).Prostaglandin E2 (PGE2) and misoprostol (EP-receptor agonist) relaxed the histamine-contracted human bronchial preparations (pD2 values, 7.13±0.07 and 6.33±0.28; Emax values, 67±04 and 57±08% of the papaverine response for PGE2 (n=14) and misoprostol (n=4), respectively). In addition, both relaxations were inhibited by AH6809 (DP/EP1/EP2-receptor antagonist; 3 μM; n=5–6).The PGE2-induced relaxations of human bronchial preparations were not modified by treatment with AH23848B (TP/EP4-receptor antagonist; 30 μM; n=4).The contracted human bronchial preparations were significantly relaxed by prostaglandin D2 (PGD2) or by BW245C a DP-receptor agonist. However, these responses did not exceed 40% of the relaxation induced by papaverine. In addition, the relaxations induced by PGD2 were significantly inhibited by treatment with a DP-receptor antagonist BWA868C (0.1 μM; n=3).These data suggest that the relaxation of human isolated bronchial preparations induced by prostanoids involved IP-, EP2- and to a lesser extent DP-receptors but not EP4-receptor.
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机译:伊洛前列素和西卡前列素(IP受体激动剂)诱导组胺(50μm)收缩的人支气管制剂中的松弛(pD2值分别为6.63±0.12和6.86±0.08; Emax值分别为罂粟碱反应的90±04和65±08%分别为伊洛前列素(n = 6)和西卡前列素(n = 3))。前列腺素E2(PGE2)和米索前列醇(EP受体激动剂)放宽了组胺收缩的人支气管制剂(pD2值,7.13±0.07和6.33±0.28) ; Emax值分别为PGE2(n = 14)和米索前列醇(n = 4)的罂粟碱反应的67±04和57±08%。此外,AH6809(DP / EP1 / EP2-受体拮抗剂;3μM; n = 5–6)均抑制了两种松弛。用AH23848B(TP / EP4-受体拮抗剂; 30μM; n = 4)。前列腺素D2(PGD2)或DP受体激动剂BW245C使收缩的人支气管制剂明显松弛。但是,这些反应未超过罂粟碱引起的松弛的40%。此外,用DP受体拮抗剂BWA868C(0.1μm; n = 3)治疗可显着抑制PGD2诱导的舒张反应。在较小程度上是DP受体,但不是EP4受体。
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