同义名 :	NE-10064 dihydrochloride; Azimilide (hydrochloride); NE 10064; Azimilide dihydrochloride
	CAS号 :	149888-94-8
	货号 :	A152509
	分子式 :	C23H30Cl3N5O3
	纯度 :	98%
	分子量 :	530.88
	MDL号 :	MFCD00918091
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Azimilide dihydrochloride is an antiarrhythmic drug with Vaughn Williams class III properties, which blocks both fast (IKr) and slow (IKs) components of the delayed rectifier cardiac potassium channel. Azimilide does not exhibit reverse-use dependence, that is, its binding characteristics and effectiveness are not related to the heart rate[3]. Azimilide prolongs cardiac refractory period in a dose-dependent manner, as manifested by increases in action potential duration, QTc interval, and effective refractory period. Azimilide does not affect PR or QRS interval and minimally affects hemodynamic properties such as blood pressure and heart rate. Azimilide has shown excellent efficacy (>85%) in suppressing supraventricular arrhythmias in a variety of dog models. It also suppressed complex ventricular arrhythmias in infarcted dogs and, in a sudden death cardiac model, decreased mortality[4]. In patients with a history of atrial fibrillation/flutter, oral azimilide controlled arrhythmias more effectively than placebo in a 6-month randomised double-blind study. At a dosage of 125 mg once daily, azimilide significantly increased the time to first symptomatic recurrence of atrial fibrillation/flutter[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.88mL 0.38mL 0.19mL	9.42mL 1.88mL 0.94mL	18.84mL 3.77mL 1.88mL

参考文献

[1]Busch AE, Eigenberger B, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123(1):23-30. [2]Fermini B, Jurkiewicz NK, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26(2):259-71. [3]Carlson M. Azimilide dihydrochloride. Expert Rev Cardiovasc Ther. 2005;3(3):387-391 [4]Karam R, Marcello S, Brooks RR, Corey AE, Moore A. Azimilide dihydrochloride, a novel antiarrhythmic agent. Am J Cardiol. 1998;81(6A):40D-46D [5]Clemett D, Markham A. Azimilide. Drugs. 2000;59(2):271-279