A-803467 is a potent and selective Nav1.8 sodium channel blocker. A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is >100-fold selective vs. human Na(v)1.2, Na(v)1.3, Na(v)1.5, and Na(v)1.7 (IC50 values >or=1 microM). Administration of A-803467 (10-30 mg/kg i.v.) reduced mechanically evoked (10-g von Frey hair) and spontaneous WDR neuronal activity in SNL rats. A-803467 also dose-dependently reduced mechanical allodynia in a variety of rat pain models. A-803467 is the first small-molecule blocker of sodium channels which showing both high potency and significant subtype-selectivity among the sodium channel family.
|Source||Sci Rep (2017). Figure 6. A-803467|
|Method||Measurement of LSG function|
|Cell Lines||Left stellate ganglion|
|Results||As shown in Fig. 6A, the ganglion neurons in the DMSO group were mostly stained positive for TH (red) and negative for TUNEL (green). However, in the high-concentration A-803467 treatment group, most ganglion neurons stained positive for both TH and TUNEL.|
|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.
|Solubility||DMSO 60 mg/mL|
A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats.
McGaraughty S, et al. J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. PMID: 18089840.
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Jarvis MF, et al. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. PMID: 17483457.
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