Wang Jianjie, Huxley Virginia H
Dept. of Medical Pharmacology and Physiology, University of Missouri, Columbia, MO 65212, USA.
Am J Physiol Heart Circ Physiol. 2006 Dec;291(6):H3094-105. doi: 10.1152/ajpheart.00526.2006. Epub 2006 Jun 30.
Little is known of the regulation of skeletal muscle microvascular exchange under resting or stimulating conditions. Adenosine (ADO) levels in skeletal muscle increase during physiological (exercise) and pathological (hypoxia, inflammation, and ischemia) conditions. Later stages of these pathologies are characterized by the loss of vascular barrier integrity. This study focused on determining which ADO receptor mediates the robust reduction in microvessel permeability to rat serum albumin (P(s)(RSA)) observed in juvenile female rats. In microvessels isolated from abdominal skeletal muscle, ADO suffusion induced a concentration-dependent reduction in arteriolar [log(IC(50)) = -9.8 +/- 0.2 M] and venular [log(IC(50)) = -8.4 +/- 0.2 M] P(s)(RSA). RT-PCR and immunoblot analysis demonstrated mRNA and protein expression of ADO A(1), A(2A), A(2B), and A(3) receptors in both vessel types, and immunofluorescence assay revealed expression of the four subtype receptors in the microvascular walls (endothelium and smooth muscle). P(s)(RSA) responses of arterioles and venules to ADO were blocked by 8-(p-sulphophenyl)theophylline, a nonselective A(1) and A(2) antagonist. An A(2A) agonist, CGS21680, was more potent than the A(1) agonist, cyclopentyladenosine, or the most-selective A(2B) agonist, 5'-(N-ethylcarboxamido)adenosine. The ability of CGS21680 or ADO to reduce P(s)(RSA) was abolished by the A(2A) antagonist, ZM241385. An adenylyl cyclase inhibitor, SQ22536, blocked the permeability response to ADO. In aggregate, these results demonstrate that, in juvenile females (before the production of the reproductive hormones), ADO enhances skeletal muscle arteriole and venule barrier function predominantly via A(2A) receptors using activation of adenylyl cyclase-signaling mechanisms.
关于静息或刺激条件下骨骼肌微血管交换的调节,目前所知甚少。在生理(运动)和病理(缺氧、炎症和缺血)状态下,骨骼肌中的腺苷(ADO)水平会升高。这些病理状态的后期阶段以血管屏障完整性丧失为特征。本研究的重点是确定哪种ADO受体介导了在幼年雌性大鼠中观察到的微血管对大鼠血清白蛋白的通透性(P(s)(RSA))的显著降低。在从腹部骨骼肌分离的微血管中,ADO灌注导致小动脉[log(IC(50)) = -9.8 +/- 0.2 M]和小静脉[log(IC(50)) = -8.4 +/- 0.2 M]的P(s)(RSA)呈浓度依赖性降低。逆转录聚合酶链反应(RT-PCR)和免疫印迹分析表明,两种血管类型中均存在ADO A(1)、A(2A)、A(2B)和A(3)受体的mRNA和蛋白表达,免疫荧光测定显示微血管壁(内皮和平滑肌)中存在四种亚型受体的表达。小动脉和小静脉对ADO的P(s)(RSA)反应被非选择性A(1)和A(2)拮抗剂8-(对-磺基苯基)茶碱阻断。A(2A)激动剂CGS21680比A(1)激动剂环戊腺苷或最具选择性的A(2B)激动剂5'-(N-乙基甲酰胺基)腺苷更有效。A(2A)拮抗剂ZM241385消除了CGS21680或ADO降低P(s)(RSA)的能力。腺苷酸环化酶抑制剂SQ22536阻断了对ADO的通透性反应。总的来说,这些结果表明,在幼年雌性(生殖激素产生之前)中,ADO主要通过A(2A)受体利用腺苷酸环化酶信号机制的激活来增强骨骼肌小动脉和小静脉的屏障功能。