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. 2022 Aug 1;13(8):895–920. doi: 10.1039/d2md00081d
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Funapide (5)55 Vixotrigine (6) AZD3161 (7)60 8: Merck62
hNaV1.1 IC50 15.2 μMb,d,46
hNaV1.5 IC50 0.084 μM 3.2 μMb,d,46 12.6 μMb 2.38 μM (Ki)c,e
hNaV1.7 IC50 0.054 μM 6.1 μMb,d,46 0.079 μMb,g 0.44 μM (Ki)c,e
Free plasma concentration 25 nM@1 mg kg−1 (CFA model)57 5 μM@23 mg kg−1h (rat formalin) 0.53 μM@1 mg kg−1h,i (rat PK)
6.0, 74 nM@0.5, 5 mg kg−1 (subchronic, CCI model)57