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 |