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RA-2 is an inhibitor of small-conductance calcium-activated potassium channel 2.3 (KCa2.3/SK3) and intermediate-conductance calcium-activated potassium channel 3.1 (KCa3.1/IK1) (IC50s = 2 and 17 nM, respectively).1 It is selective for these channels over KCa1.1/BK1, voltage-gated potassium channel 1.2 (Kv1.2), Kv1.3, Kv7.4, human-ether-a-go-go (hERG), also known as Kv11.1, and the inward-rectifier potassium channel (Kir), but also inhibits KCa2.1 and KCa2.2 by 96 and 90%, respectively, at 1 µM. RA-2 (1 µM) inhibits bradykinin-induced relaxation of porcine coronary artery rings precontracted with the TP receptor agonist U-46619 (Item No. 16450). It decreases heart rate, but not mean arterial blood pressure, in mice when administered at a dose of 30 mg/kg.
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1. A novel pan-