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. 2023 Jan 9;66(2):1583–1600. doi: 10.1021/acs.jmedchem.2c01830

Table 5. TRPA1 Potency and Metabolic Stability of Compounds 18 and 34ega.

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
a

Compound 18: fu% rat = 6%; brain= 4.3%; mouse = 8.1%; human = 12%, guinea pig = 9.7%.