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Activation of B2 bradykinin receptors by neurotensin

机译:神经降压素激活B2缓激肽受体

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Many previous reports suggested that relatively high concentrations of neurotensin were required to exert its effects on neurotransmitter secretion. The neurotensin binding sites, which recognize high concentrations of neurotensin, were characterized in rat pheochromocytoma (PC12) cells. When PC12 cells were treated with neurotensin, [H-3]norepinephrine secretion and elevation of cytosolic calcium were evoked at EC50 values of 59 +/- 4 and 37 +/- 7 muM, respectively. Both calcium release and inositol 1,4,5-trisphosphate (IP3) production induced by neurotensin suggested involvement of phospholipase C. Experiments with simultaneous or sequential treatment with neurotensin and bradykinin suggested that neurotensin and bradykinin act on the same binding sites. Furthermore, both inhibition of bradykinin- and neurotensin-induced calcium rises by bradykinin receptor antagonists with similar IC50 values and receptor binding analysis using [H-3]bradykinin confirmed that neurotensin directly binds to B2 bradykinin receptors. The data suggest that neurotensin binds and activates the B2 bradykinin receptors. (C) 2002 Elsevier Science Inc. All rights reserved. [References: 37]
机译:以前的许多报告表明,需要较高浓度的神经降压素来发挥其对神经递质分泌的作用。在大鼠嗜铬细胞瘤(PC12)细胞中表征了识别高浓度神经降压素的神经降压素结合位点。当用神经降压素处理PC12细胞时,在EC50值分别为59 +/- 4和37 +/- 7μM时引起[H-3]去甲肾上腺素的分泌和胞质钙的升高。神经降压素诱导的钙释放和肌醇1,4,5-三磷酸(IP3)的产生均提示磷脂酶C参与。神经降压素和缓激肽同时或顺序治疗的实验表明,神经降压素和缓激肽作用于相同的结合位点。此外,具有相似IC50值的缓激肽受体拮抗剂对缓激肽和神经降压素诱导的钙的抑制作用均得到提高,并且使用[H-3]缓激肽的受体结合分析证实,神经降压素直接与B2缓激肽受体结合。数据表明神经降压素结合并激活B2缓激肽受体。 (C)2002 Elsevier Science Inc.保留所有权利。 [参考:37]

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