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,
Application Amlodipine besylate is a L-type calcium channel blocker which may be used for the treatment of angina pectoris and hypertension. Amlodipine also inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats. Biochem/physiol Actions Amlodipine is an L-type calcium channel blocker. Amlodipine belongs to a class of cardiovascular drugs, which act at the voltage gated calcium channel of the CaV1, or L-type, class. Amlodipine also has antihypertensive and antianginal effects. Its activity resides mainly in the (-)-isomer. Amlodipine inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.
Harmful (Xn)