From:  Phenylalanine-derived β-lactam TRPM8 antagonists: revisiting configuration and new benzoyl derivatives

Antagonist activity of β-lactams 11a and 12a in hTRPM8 (Ca2+ microfluorometry) and electrophysiology in rTRPM8 channels (patch-clamp assays). Activation is induced by 100 µM menthol

CompoundCa2+ microfluorometry assaysPatch-clamp assay
rTRPM8, IC50 (µM)hTRPM8, IC50 (µM)95% confidence intervalsrTRPM8, IC50 (µM)95% confidence intervals
1a1.06 ± 1.211.74 ± 1.191.23 to 2.450.60 ± 1.660.20 to 1.76
11a2.49 ± 1.454.33 ± 1.133.39 to 5.550.51 ± 1.330.28 to 0.92
12a1.14 ± 1.532.08 ± 1.201.45 to 3.00NDaND
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a Solubility issue in the Patch-Clamp buffer. ND: no data. IC50: concentration exerting a half-maximal inhibition; rTRPM8: rat transient receptor potential melastatin, subtype 8; hTRPM8: human transient receptor potential melastatin, subtype 8