biological activity | NP118809 is an effective n-type calcium channel (N-type calcium channel) blocker with an IC50 value of 0.11 μM; At the same time, it can weakly inhibit l-type calcium channel (L-type calcium channel) with an IC50 value of 12.2 μM. |
target | N-Type Ca 2 + Channel 0.11 μM (IC 50 ) L-type calcium channel 12.2 μM (IC 50 ) |
in vitro study | NP118809 is a potent N-type calcium channel blocker, with an IC 50 of 0.11 μ M; Also inhibits L-type calcium channel with an IC 50 of 12.2 μ M. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC 50 of 7.4 μ m. |
in vivo study | NP118809 (25 mg/kg, I. p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model. NP118809 (30 mg/kg, P. o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibition of thermal hyperalgesia in the rat spinal nerve ligation model. |