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。
| 生物活性 | Ivabradine is a potent and orally activeHCN (hyperpolarization-activated cyclic nucleotide-gated) channelblocker 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]. |
体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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