NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model[1]. 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[2].
In Vitro
NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also inhibits L-type calcium channel with an IC50 of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC50 of 7.4 μM[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Zamponi GW, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72.
[2]. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83.
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