Inhibition of NaV1.7: the possibility of ideal analgesics

. 2022 Aug 1;13(8):895–920. doi: 10.1039/d2md00081d


	AMG8379 (25)⁸⁶	26: Amgen⁸⁸	27: Amgen⁸⁸	28: Pfizer⁸⁹
hNa_V1.1 IC₅₀	>14 000 nM^c^,ⁿ	7300 nM^e^,^o	17 000 nM^c	314 nM^c^,^d
hNa_V1.5 IC₅₀	>14 000 nM^c^,ⁿ	16 000 nM^e^,^o	12 000 nM^c	2592 nM^c^,^d
hNa_V1.7 IC₅₀	8.5 nM^c^,^h, 3.2 nM^c^,ⁿ	140 nM^e^,^o	17 nM^c	0.01 nM^c^,^d
Mouse Na_V1.7 IC₅₀	18.6 nM^c^,^h, 16.8 nM^c^,ⁿ	180 nM^c^,^o	36 nM^c	<0.1 nM^c^,^d
Mouse PPB^b	99.83%	96.45%	98.84%	99.719%
Na_V1.7 coverage in plasma@efficacious dosage^a	5.3-Fold@30 mg kg⁻¹ (mouse histamine)	28-Fold@60 mg kg⁻¹ (mouse histamine)	45-Fold@300 mg kg⁻¹ (mouse histamine)	>62.5-Fold@5.4 mg kg⁻¹ (i.v.) (mouse formalin)
	23-Fold@100 mg kg⁻¹ (UVB-induced thermal hyperalgesia in mice)
	21-Fold@100 mg kg⁻¹ (mouse capsaicin)