241499-17-2

IC50: 0.7 μM (N-type calcium channels)

N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC ₅₀ =0.7 μM). N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds.

N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED ₅₀ =4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED ₅₀ =12 mg/kg, po). A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg. Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20).