RQ-00203078

RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC₅₀s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC₅₀ > 30 µM), TRPA1 (IC₅₀ > 10 µM), TRPV4 (IC₅₀ = 10 µM), or TRPM2 channels (IC₅₀ > 10 µM).¹ It attenuates icilin-induced wet-dog shakes in rats (ED₅₀ = 0.65 mg/kg) after oral administration.¹ RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.² TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas.

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1. Ohmi, M., Shishido, Y., Inoue, T., et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg. Med. Chem. Lett. 24(23), 5364-5368 (2014).

2. Okamoto, Y., Ohkubo, T., Ikebe, T., et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int. J. Oncol. 40(5), 1431-1440 (2016).