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首页> 外文期刊>Cardiovascular therapeutics >Imidazoline Antihypertensive Drugs: Selective I 1-Imidazoline Receptors Activation
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Imidazoline Antihypertensive Drugs: Selective I 1-Imidazoline Receptors Activation

机译：咪唑啉降压药：选择性I 1-咪唑啉受体激活

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Involvement of imidazoline receptors (IR) in the regulation of vasomotor tone as well as in the mechanism of action of some centrally acting antihypertensives has received tremendous attention. To date, pharmacological studies have allowed the characterization of three main imidazoline receptor classes, the I 1-imidazoline receptor which is involved in central inhibition of sympathetic tone to lower blood pressure, the I 2-imidazoline receptor which is an allosteric binding site of monoamine oxidase B (MAO-B), and the I 3-imidazoline receptor which regulates insulin secretion from pancreatic β-cells. All three imidazoline receptors represent important targets for cardiovascular research. The hypotensive effect of clonidine-like centrally acting antihypertensives was attributed both to α 2-adrenergic receptors and nonadrenergic I 1-imidazoline receptors, whereas their sedative action involves activation of only α 2-adrenergic receptors located in the locus coeruleus. Since more selective I 1-imidazoline receptors ligands reduced incidence of typical side effects of other centrally acting antihypertensives, there is significant interest in developing new agents with higher selectivity and affinity for I 1-imidazoline receptors. The selective imidazoline receptors agents are also more effective in regulation of body fat, neuroprotection, inflammation, cell proliferation, epilepsy, depression, stress, cell adhesion, and pain. New agonists and antagonists with high selectivity for imidazoline receptor subtypes have been recently developed. In the present review we provide a brief update to the field of imidazoline research, highlighting some of the chemical diversity and progress made in the theoretical studies of imidazoline receptor ligands.
机译：咪唑啉受体（IR）在调节血管舒缩张力以及某些中枢性降压药的作用机制中的作用已引起极大关注。迄今为止，药理学研究已经可以鉴定出三种主要的咪唑啉受体类别：I 1-咪唑啉受体，其对降血压的交感神经有中枢抑制作用; I 2-咪唑啉受体，其为单胺的变构结合位点。氧化酶B（MAO-B）和I 3-咪唑啉受体，该受体调节胰腺β细胞分泌的胰岛素。三种咪唑啉受体均代表心血管研究的重要目标。可乐定样的中枢性降压药的降压作用既归因于α2-肾上腺素受体和非肾上腺素I 1-咪唑啉受体，而其镇静作用仅涉及位于蓝斑蓝斑的α2-肾上腺素受体的激活。由于更具选择性的I 1-咪唑啉受体配体降低了其他中枢性降压药典型副作用的发生率，因此，人们对开发对I 1-咪唑啉受体具有更高选择性和亲和力的新型药物产生了浓厚兴趣。选择性咪唑啉受体剂在调节体内脂肪，神经保护，炎症，细胞增殖，癫痫，抑郁，压力，细胞粘附和疼痛方面也更有效。最近已经开发了对咪唑啉受体亚型具有高选择性的新型激动剂和拮抗剂。在本综述中，我们对咪唑啉研究领域进行了简要更新，重点介绍了咪唑啉受体配体的理论研究中的一些化学多样性和进展。

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