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Table 1 Summary of inhibition of the TRPM8-wt channel.

From: Differential role of the menthol-binding residue Y745 in the antagonism of thermally gated TRPM8 channels

Compound

IC50 cold (μM)

IC50 menthol (μM)

BCTC

0.68 ± 0.06a (CI)

0.54 ± 0.04a (EP)

0.47 ± 0.01b (CI)

0.34 ± 0.04b (EP)

SKF96365

1.0 ± 0.2a (CI)

0.8 ± 0.1a (EP)

3 ± 1b (CI)

Capsazepine

12 ± 2d (CI)

18 ± 1c (FLIPR)

Clotrimazole

8 ± 1d (CI)

1.2e (EP)

Econazole

0.42 ± 0.07d (CI)

N/A

Imidazole

>> 1000

N/A

  1. Inhibitory potency of various blockers at the cold- or 100 μM menthol-activated TRPM8-wt channel as measured by calcium imaging (CI), a fluorometric imaging plate reader assay (FLIPR) or electrophysiology (EP). Data are from: a[26]; bmodified from [25]; c[24]; dthis work; e[27]. Whole-cell patch-clamp data are given at +80 mV, except for e, where the block was estimated at +50 mV.
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Molecular Pain

ISSN: 1744-8069

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