Tam Christina, Brain Susan D
Centre for Cardiovascular Biology and Medicine, New Hunt's House, Guy's Campus, King's College, London, SE1 1UK.
J Mol Neurosci. 2004;22(1-2):117-24. doi: 10.1385/JMN:22:1-2:117.
The potent neuropeptide vasodilator, calcitonin gene-related peptide (CGRP), and the vasoactive peptide adrenomedullin (AM) are structurally related. Evidence from our laboratory has demonstrated that these peptides have potent microvascular actions of relevance to cardiovascular and inflammatory effects in health and disease. We wish to further investigate the actions of these peptides through studies in genetically modified mice. We have developed techniques to enable the quantitative analysis of CGRP and AM responses in the mouse microvasculature. A mouse isolated mesentery system was developed that measures changes in perfusion pressure used as an index of microvascular relaxation in the precontracted mesenteric microvascular bed. Bolus injections of CGRP and AM caused dose-dependent decreases in perfusion pressure that were proportional to vascular relaxation. An in vivo mouse skin assay was also used in which agents were injected intradermally into the dorsal skin. The effects of these agents was assessed by the extravascular accumulation of intravenously injected 125I-albumin for their ability to potentiate plasma extravasation induced by a mediator of increased microvascular permeability. CGRP and AM are not directly active in this assay, because it does not directly measure blood flow. However, the vasodilators acted in a potent and dose-dependent manner to significantly potentiate edema formation. The results demonstrate the potent activity of CGRP and the activity (although 100- to 300-fold less potent) of AM. Furthermore, the results demonstrate the increased potency of CGRP in the microvasculature when compared with the structurally distinct peptide VIP and PGE1.
强效神经肽血管舒张剂降钙素基因相关肽(CGRP)与血管活性肽肾上腺髓质素(AM)在结构上相关。我们实验室的证据表明,这些肽具有与健康和疾病中的心血管及炎症效应相关的强效微血管作用。我们希望通过对转基因小鼠的研究进一步探究这些肽的作用。我们已开发出技术,能够对小鼠微血管中CGRP和AM的反应进行定量分析。我们建立了一种小鼠离体肠系膜系统,该系统可测量灌注压力的变化,以此作为预收缩肠系膜微血管床微血管舒张的指标。静脉推注CGRP和AM会导致灌注压力呈剂量依赖性降低,且与血管舒张成正比。我们还使用了一种体内小鼠皮肤试验,将药物皮内注射到背部皮肤中。通过静脉注射125I - 白蛋白的血管外蓄积来评估这些药物增强由微血管通透性增加介质诱导的血浆外渗的能力,从而评估其效果。CGRP和AM在该试验中并非直接起作用,因为它不直接测量血流量。然而,这些血管舒张剂以强效且剂量依赖性的方式显著增强水肿形成。结果证明了CGRP的强效活性以及AM的活性(尽管效力低100至300倍)。此外,结果表明与结构不同的肽血管活性肠肽(VIP)和前列腺素E1(PGE1)相比,CGRP在微血管中的效力更高。