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Pharmacological Properties of the Central Antihypertensive Agent, Moxonidine

机译：中央降压药莫索尼定的药理特性

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The sympathetic nervous system plays a central role in the pathophysiology not only of hypertension and other cardiovascular diseases but also metabolic disorders including disturbances of glucose and lipid homeostasis. A centrally acting sympathetic agent is therefore attractive not only for lowering blood pressure, but also intervening with multiple disease processes. Older agents such as clonidine and guanabenz have numerous side effects, including sedation and dry mouth that limit their acceptability to patients. Moxonidine and the related agent rilmenidine have greatly reduced side effects, because they have reduced activity at the α 2-adrenergic receptors that mediate these undesirable actions. Instead, moxonidine and rilmenidine act primarily through a novel cellular site, termed the I 1-imidazoline receptor. The molecular biology of the I 1-imidazoline receptor protein has recently been described, and the cell signaling pathways linked to this protein have been characterized. Moxonidine has unique effects on a number of cell types through this unusual cellular site of action. There are multiple therapeutic implications of these cellular actions, especially for metabolic syndrome and its associated derangements in glucose and lipid metabolism. Finally, the clinical trials that seemed to identify an unfavorable outcome in severe heart failure are dissected and critiqued. We conclude that moxonidine and future successors to this agent could be of great value in treating multiple chronic diseases.
机译：交感神经系统不仅在高血压和其他心血管疾病的病理生理中起着重要作用，而且在包括葡萄糖和脂质体内平衡紊乱在内的代谢紊乱中也起着重要作用。因此，中枢性交感剂不仅对降低血压具有吸引力，而且还可以干预多种疾病。诸如可乐定和瓜纳本斯等较老的药物具有许多副作用，包括镇静作用和口干，这限制了它们对患者的接受性。莫索尼定和相关药物瑞美替丁具有大大降低的副作用，因为它们对介导这些不良作用的α2-肾上腺素能受体的活性降低。取而代之的是，莫索尼定和瑞美尼定主要通过一个称为I 1-咪唑啉受体的新型细胞部位起作用。最近已经描述了I 1-咪唑啉受体蛋白的分子生物学，并且已经表征了与该蛋白连接的细胞信号传导途径。莫索尼定通过这种异常的细胞作用位点对多种细胞类型具有独特的作用。这些细胞作用有多种治疗意义，尤其是对于代谢综合症及其相关的葡萄糖和脂质代谢紊乱。最后，对似乎确定了严重心力衰竭不良结果的临床试验进行了解剖和批判。我们得出的结论是，莫索尼定和该药物的未来继承者在治疗多种慢性疾病方面可能具有巨大价值。

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