AVE-0118

AVE-0118 is a nonselective Kv1.5 blocker with an IC50 of 1.1 μM. AVE-0118 is a multichannel inhibitor with weak, micromolar activity against Kv1.5 and other ion channels. It is inactive against IKs, IKATP, and L-type Ca+ channels.

AVE-0118 is shown to be a Kv1.5 blocker (IC₅₀ = 1.1 uM) with moderate selectivity versus I_to (3.4 uM), I_Kr (8.4 uM), and I_KAch (4.5 uM) and good selectivity versus I_Ks, I_K1, I_KATP^[1].
AVE-0118 (10 μM) significantly potentiates the electrical field stimulation (EFS)-induced neurogenic type of contractions^[2].

AVE-0118 reduces the inducibility of AF in goats with remodeled atria at a dose of 3 mg/kg and did not prolong QTc up to 5 mg/kg^[1].

References:
[1]. Bilodeau MT, et al. Kv1.5 blockers for the treatment of atrial fibrillation: approaches to optimization of potency and selectivity and translation to in vivo pharmacology. Curr Top Med Chem. 2009;9(5):436-51.
[2]. Kun A, et al. Neurogenic contraction induced by the antiarrhythmic compound, AVE 0118, in rat small mesenteric arteries. Basic Clin Pharmacol Toxicol. 2014 Oct;115(4):315-20.