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. Author manuscript; available in PMC: 2019 Feb 1.
Published in final edited form as: Bioorg Chem. 2017 Dec 30;76:510–527. doi: 10.1016/j.bioorg.2017.12.024

Table 8.

Metabolic stability of sEH inhibitors with substituents in bridgehead positions of adamantane against human microsomes (HLM).

# Amount remaining after 30
minutes in contact with HLM (%)
T½ (min) Clint*
(µL.min−1.mg−1)
− NADPH + NADPH
147136 97 ± 8 69 ± 2 56 12
1b 95 ± 3 64 ± 6 54 ± 3 13 ± 1
2b 100 ± 3 8 ± 2 8 ± 1 84 ± 6
3b 95 ± 4 0.7 ± 0.2 3.5 ± 0.3 196 ± 2
*

Intrinsic clearance