Research Area: Cardiovascular Disease
Biological Activity:
Amlodipine(Norvasc) is a long-acting calcium channel blocker with an IC50 of 1.9 nM.Amlodipine specifically inhibited bTREK-1 in a concentration-dependent manner with an IC50 of 0.43μM.At concentrations that produced near complete block of bTREK-1, amlodipine inhibited voltage-gated Kv1.4 K+ and T-type Ca2+currents in AZF cells by less than 10%. [1]Amlodipine was twice as potent as nifedipine at inhibiting Ca2+-induced contractions in depolarised rat aorta (IC50 1.9 nM vs. 4.1 nM) but, unlike nifedipine, displayed a very slow onset of action.Amlodipine also inhibited 35 mM KCl-induced contractions of pig coronary artery rings (IC50 = 2.2 x 10-8 M) and human coronary artery rings (IC50 = 2.1 x 10-8 M). [2]Hypertension (HTN) or high blood pressure is a cardiac chronic medical condition in which the systemic arterial blood pressure is elevated.Amlodipine besylate has been used for treating hypertension in Phase III. [3]Amlodipine besylate is originally developed by Pfizer.References on Amlodipine besylate (Norvasc)[1] JPET, 2007, 323:39–48, |