Potassium Canrenoate

Potassium canrenoate是醛固酮受体的竞争性拮抗剂[1]。

醛固酮是一个类固醇激素，在通过增加肾脏内离子和水的重吸收而调节血压的过程中起着重要作用。

在培养的大鼠和人类细胞中，Potassium canrenoate以剂量依赖的方式产生基因毒性[2]。

对雄性Wistar鼠注射异丙肾上腺素(400 mg/kg)，心脏和左心室的重量显著增加。而Potassium canrenoate (20 mg/kg/d)消除了这一增长。Potassium canrenoate显著降低由异丙肾上腺素诱导产生的纤维化[1]。在30个重要的高血压药物中，Potassium canrenoate减少红细胞内Na+含量，增加Na-K泵[3]。在15个原发性醛固酮增多症患者中，Potassium canrenoate使醛固酮/血浆肾素活性(PRA)的比率正常化[4]。

参考文献：
[1]. Bos R, Mougenot N, Médiani O, et al. Potassium canrenoate, an aldosterone receptor antagonist, reduces isoprenaline-induced cardiac fibrosis in the rat. J Pharmacol Exp Ther, 2004, 309(3): 1160-1166.
[2]. Martelli A, Mattioli F, Carrozzino R, et al. Genotoxicity testing of potassium canrenoate in cultured rat and human cells. Mutagenesis, 1999, 14(5): 463-472.
[3]. Niutta E, Cusi D, Colombo R, et al. Antihypertensive effect of captopril, canrenoate potassium, and atenolol. Relations with red blood cell sodium transport and renin. Am J Hypertens, 1988, 1(4 Pt 1): 364-371.
[4]. Armanini D, Scaroni C, Mattarello MJ, et al. Idiopathic primary hyperaldosteronism: normalization of plasma aldosterone after one month withdrawal of long-term therapy with aldosterone-receptor antagonist potassium canrenoate. J Endocrinol Invest, 2005, 28(3): 236-240.