Table 5. TRPA1 Potency and Metabolic Stability of Compounds 18 and 34e–ga.
compound | hTRPA1 IC50 [nM] | rTRPA1 IC50 [nM] | rHeps [L/h/kg] | hLMs [L/h/kg] | log D (HPLC) |
---|---|---|---|---|---|
18 | 16 | 63 | 2.4 | 0.38 | 3.0 |
34e | 21 | 200 | 2.3 | 0.48 | n.d. |
34f | 55 | 680 | 3.2 | 0.68 | 3.4 |
34g | 41 | 650 | 1.8 | 0.44 | 3.8 |
Compound 18: fu% rat = 6%; brain= 4.3%; mouse = 8.1%; human = 12%, guinea pig = 9.7%.