AVE 0118 hydrochloride

• CAT Number: I047602
• CAS Number: 2108821-80-1
• Molecular Formula: C30H29N3O3.HCl
• Molecular Weight: 516.03
• Purity: ≥95%
• IUPAC Name: 2-[2-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]phenyl]-N-(2-pyridin-3-ylethyl)benzamide;hydrochloride
• InChI: InChI=1S/C30H29N3O3.ClH/c1-36-25-14-12-22(13-15-25)19-29(34)33-21-24-8-2-3-9-26(24)27-10-4-5-11-28(27)30(35)32-18-16-23-7-6-17-31-20-23;/h2-15,17,20H,16,18-19,21H2,1H3,(H,32,35)(H,33,34);1H
• SMILES: COC1=CC=C(C=C1)CC(=O)NCC2=CC=CC=C2C3=CC=CC=C3C(=O)NCCC4=CN=CC=C4.Cl

Potassium channel blocker. AVE0118 caused concentration-dependent inhibition of Kv1.5 (IKur), Kv4.3 (Ito), Kir3.4 (IKAch), and IKr currents (IC50 values 6.2 μM, 3.4 μM, 4.5 μM, and 10 μM resp.). A potent and atrium selective antiarrhythmic compound with no apparent effect on ventricular repolarization. Noteworthy, the atrial selective and dose-dependent prolongation of atrial refractoriness (ERP) by AVE 0118 has been claimed to be an inhibitory effect of sodium channel activity in an atrial-selective manner, and may therefor contribute to anti-AF properties of AVE0118.
KEYWORDS: AVE 0118 hydrochloride | IKur channel blocker | AVE0118 | AVE-0118 | CAS [2108821-80-1] | [498577-53-0] | Potassium | Kv1.5 | Kv4.3 | Kir4.3 | Blocker | Ion Channels | KCNA5 | KCND3 | KCNJ5 | KCNE1 | Voltage gated | Antiarrhythmic | Atrial | Refractoriness | ERP

Reference

H. Gögelein et al. Effects of the atrial antiarrhythmic drug AVE0118 on cardiac ion channels. Naun. Schmiedebergs Arch. Pharmacol. 2004, 370, 183-192.

 

K.J. Wirth et al. Atrial effects of the novel K+-channel-blocker AVE0118 in anesthetized pigs. Cardiovascular Res. 2003, 60, 298-306. 

 

A. Burashnikov et al. Atrial-selective prolongation of refractory period with AVE0118 is due principally to inhibition of sodium channel activity. J. Cardiovasc. Pharmacol. 2012, 59, 539-546.