NP-118809 (39-1B4) is a potent N-type calcium channel blockers (IC50= 0.11 uM) which has good selectivity over L-type calcium channels. NP-118809 exhibites increased N-type channel blockade (IC50=0.11 uM) and is 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM). NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||Bioorg Med Chem Lett (2010). Figure 3. NP118809|
|Results||Figure 2 shows that up on intraperitoneal (ip) administration both NP118809 and NP078585 (25 mg/kg) both exhibited significant analgesic activity in the phase IIA portions of the rat formalin model.|
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Zamponi GW, et al. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. PMID: 19815411.
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