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Synonyms: A-293 | A293 | AVE-1231
Compound class: Synthetic organic
Comment: AVE1231 is a K2P3.1 (TASK-1) channel blocker [2-3]. It was originally reported as a inhibitor of hKv1.5 currents [1,4], and was being developed as an atrial-selective drug therapy by Sanofi-Aventis for the treatment of atrial fibrillation, but the programme was terminated at Phase 1.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Ehrlich JR, Ocholla H, Ziemek D, Rütten H, Hohnloser SH, Gögelein H. (2008)
Characterization of human cardiac Kv1.5 inhibition by the novel atrial-selective antiarrhythmic compound AVE1231.
J Cardiovasc Pharmacol, 51 (4): 380-7. [PMID:18427281]
2. Shvetsova AA, Gaynullina DK, Schmidt N, Bugert P, Lukoshkova EV, Tarasova OS, Schubert R. (2020)
TASK-1 channel blockade by AVE1231 increases vasocontractile responses and BP in 1- to 2-week-old but not adult rats.
Br J Pharmacol, 177 (22): 5148-5162. [PMID:32860629]
3. Wiedmann F, Kiper AK, Bedoya M, Ratte A, Rinné S, Kraft M, Waibel M, Anad P, Wenzel W, González W et al.. (2019)
Identification of the A293 (AVE1231) Binding Site in the Cardiac Two-Pore-Domain Potassium Channel TASK-1: a Common Low Affinity Antiarrhythmic Drug Binding Site.
Cell Physiol Biochem, 52 (5): 1223-1235. [PMID:31001961]
4. Wirth KJ, Brendel J, Steinmeyer K, Linz DK, Rütten H, Gögelein H. (2007)
In vitro and in vivo effects of the atrial selective antiarrhythmic compound AVE1231.
J Cardiovasc Pharmacol, 49 (4): 197-206. [PMID:17438404]