AP-18 is a novel ANKTM1 (TRPA1 channel) blocker (CHO cells, IC50= 3.1 μM; human and mouse cell lines, IC50= 4.5 μM). It blocks cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation.
Petrus et al (2007) A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Mol.Pain 3 40. Chen et al (2009) Pore dilation occurs in TRPA1 but not in TRPM8 channels. Mol.Pain 5 3. Taylor-Clark et al (2009) Nitrooleic acid, an endogenous product of nitrative stress, activates nociceptive sensory nerves via the direct activation of TRPA1. Mol.Pharmacol. In press.
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