Ivabradine 是一种有效且具有口服活性的 HCN (超极化激活的环核苷酸门控) 通道阻滞剂，可抑制心脏起搏器电流 (If)。Ivabradine 以剂量依赖性降低心率而不改变血压。Ivabradine 具有抗惊厥、抗缺血和抗心绞痛活性。

Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity [1] [2] [3] [4].

Ivabradine (1, 10, 20 mg/kg; i.p.) shows anticonvulsant and neuroprotective action in mice [3]. Ivabradine (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities [4]. Animal Model: 25-30 g, 6 weeks male Swiss mice [3] Dosage: 1, 10, 20 mg/kg Administration: I.p.; for 3 days Result: Attenuated PTZ- and PICRO-induced seizures while presented an antioxidant effect in all brain areas studied, and reduced cleaved caspase-3 expression in the CA1 and DG region of PICRO- and PTZ-treated mice, respectively. Animal Model: 3-4 months transgenic (TG) mice with cardiac-restricted overexpression of b2AR [4] Dosage: 5, 10, 20 mg/kg Administration: P.o; daily for 1 weeks Result: Reduced the maximal HR increase in response to the b-agonist isoproterenol, without modifying the response of contractile parameters at 10 mg/kg.

155974-00-8

C27H36N2O5

468.59

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years