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编 号:F185649
分子式:C27H36N2O5
分子量:468.59
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生物活性:
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.

体内研究:
Ivabradine (1, 10, 20 mg/kg; i.p.) shows anticonvulsant and neuroprotective action in mice.Ivabradine (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities.Animal Model:25-30 g, 6 weeks male Swiss mice
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 allbrain 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
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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