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AVE 0118 hydrochloride
- Parent CAS: 498577-53-0
- Soluble in water and DMSO
- MF: C30H29N3O3.HCl
- MW: 516.03
Description
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.
More Information
| Parent CAS No. | 498577-53-0 |
|---|---|
| Chemical Name | 2'-((2-(4-methoxyphenyl)acetamido)methyl)-N-(2-(pyridin-3-yl)ethyl)biphenyl-2-carboxamide hydrochloride |
| SMILES | C1(C2=CC=CC=C2CNC(CC2=CC=C(OC)C=C2)=O)=CC=CC=C1C(NCCC1=CC=CN=C1)=O.Cl |
| MFCD | N.A. |
| 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 |
| InChiKey | VLHHQGXIOINJIC-UHFFFAOYSA-N |
| CID | 91826504 |
| Short Description | IKur channel blocker |
References
- 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.
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