Inserm CIC1418, service d'hypertension artérielle et DMU CARTE, HEGP, université de Paris, AP-HP, 20-40, rue Leblanc, 75015 Paris, France.
Ann Endocrinol (Paris). 2021 Jun;82(3-4):179-181. doi: 10.1016/j.ando.2020.03.009. Epub 2020 May 27.
Blocking the mineralocorticoid receptor (MR) is one of the most effective ways of reducing blood pressure in patients with resistant hypertension and improving cardiovascular prognosis in patients with heart failure with reduced ejection fraction and left ventricular dysfunction after myocardial infarction. Blockade of the biological effects of aldosterone has mostly been achieved with spironolactone and eplerenone, the two steroidal MR antagonists currently on the market. Development of new non-steroidal dihydropyridine-based third- and fourth-generation MR antagonists is ongoing. These antagonists are highly selective for the MR, but have no effect on the glucocorticoid, androgen, progesterone and estrogen receptors, in contrast with spironolactone.
阻断盐皮质激素受体（MR）是降低耐药性高血压患者血压和改善射血分数降低的心力衰竭以及心肌梗死后左心室功能障碍患者心血管预后的最有效方法之一。醛固酮的生物效应阻断主要通过螺内酯和依普利酮来实现，这两种甾体 MR 拮抗剂是目前市场上的产品。新型非甾体二氢吡啶类第三代和第四代 MR 拮抗剂的开发正在进行中。与螺内酯不同，这些拮抗剂对 MR 具有高度选择性，但对糖皮质激素、雄激素、孕激素和雌激素受体没有作用。
