Aprikalim  (Synonyms: RP 52891)

Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guinea pig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions^[1].

268.40

C₁₂H₁₆N₂OS₂

132562-26-6

S=C([C@]1(C2=CC=CN=C2)CCCC[S@]1=O)NC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. D Thuringer, et al. Time-dependent fading of the activation of KATP channels, induced by aprikalim and nucleotides, in excised membrane patches from cardiac myocytes. Br J Pharmacol. 1995 May;115(1):117-27.  [Content Brief]