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利钠肽诱导心脏交感神经元儿茶酚胺释放:组胺 H3 和 H4 受体激活的抑制作用。

Natriuretic peptide-induced catecholamine release from cardiac sympathetic neurons: inhibition by histamine H3 and H4 receptor activation.

机构信息

Department of Pharmacology, Weill Cornell Medical College, New York, NY 10065, USA.

出版信息

J Pharmacol Exp Ther. 2012 Dec;343(3):568-77. doi: 10.1124/jpet.112.198747. Epub 2012 Aug 24.

Abstract

We reported previously that natriuretic peptides, including brain natriuretic peptide (BNP), promote norepinephrine release from cardiac sympathetic nerves and dopamine release from differentiated pheochromocytoma PC12 cells. These proexocytotic effects are mediated by an increase in intracellular calcium secondary to cAMP/protein kinase A (PKA) activation caused by a protein kinase G (PKG)-mediated inhibition of phosphodiesterase type 3 (PDE3). The purpose of the present study was to search for novel means to prevent the proadrenergic effects of natriuretic peptides. For this, we focused our attention on neuronal inhibitory Gα(i/o)-coupled histamine H(3) and H(4) receptors. Our findings show that activation of neuronal H(3) and H(4) receptors inhibits the release of catecholamines elicited by BNP in cardiac synaptosomes and differentiated PC12 cells. This effect results from a decrease in intracellular Ca(2+) due to reduced intracellular cAMP/PKA activity, caused by H(3) and H(4) receptor-mediated PKG inhibition and consequent PDE3-induced increase in cAMP metabolism. Indeed, selective H(3) and H(4) receptor agonists each synergized with a PKG inhibitor and a PDE3 activator in attenuating BNP-induced norepinephrine release from cardiac sympathetic nerve endings. This indicates that PKG inhibition and PDE3 stimulation are pivotal for the H(3) and H(4) receptor-mediated attenuation of BNP-induced catecholamine release. Cardiac sympathetic overstimulation is characteristic of advanced heart failure, which was recently found not to be improved by the administration of recombinant BNP (nesiritide), despite the predicated beneficial effects of natriuretic peptides. Because excessive catecholamine release is likely to offset the desirable effects of natriuretic peptides, our findings suggest novel means to alleviate their adverse effects and improve their therapeutic potential.

摘要

我们之前曾报道过,利钠肽,包括脑利钠肽(BNP),可促进心脏交感神经释放去甲肾上腺素和多巴胺从分化的嗜铬细胞瘤 PC12 细胞释放。这些出胞作用是通过 cAMP/蛋白激酶 A(PKA)激活引起的细胞内钙增加介导的,这是由蛋白激酶 G(PKG)介导的磷酸二酯酶 3(PDE3)抑制引起的。本研究的目的是寻找新的方法来预防利钠肽的促肾上腺素作用。为此,我们将注意力集中在神经元抑制性 Gα(i/o)-偶联组氨酸 H(3)和 H(4)受体上。我们的研究结果表明,激活神经元 H(3)和 H(4)受体可抑制 BNP 在心脏突触小体和分化的 PC12 细胞中引起的儿茶酚胺释放。这种作用是由于细胞内 cAMP/PKA 活性降低引起的细胞内 Ca(2+)减少所致,这是由 H(3)和 H(4)受体介导的 PKG 抑制和随后的 PDE3 诱导的 cAMP 代谢增加引起的。事实上,选择性 H(3)和 H(4)受体激动剂各自与 PKG 抑制剂和 PDE3 激活剂协同作用,可减弱 BNP 诱导的心脏交感神经末梢去甲肾上腺素释放。这表明 PKG 抑制和 PDE3 刺激对于 H(3)和 H(4)受体介导的 BNP 诱导儿茶酚胺释放的抑制至关重要。心脏交感神经过度刺激是晚期心力衰竭的特征,最近发现尽管利钠肽具有预期的有益作用,但给予重组 BNP(奈西立肽)并不能改善这种情况。因为过量的儿茶酚胺释放可能会抵消利钠肽的理想作用,我们的研究结果表明了新的方法来减轻它们的不良影响并提高它们的治疗潜力。

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