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PF 05105679 is a selective TRPM8 blocker (IC50 = 103 nM) that exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. PF 05105679 reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. This compound is orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 05105679 is reviewed.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Andrews et al (2015) Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain. ACS Med.Chem.Lett. 6 419 PMID: 25893043
Winchester et al (2014) Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J.Pharmacol.Exp.Ther. 351 259 PMID: 25125580
Keywords: PF 05105679, PF 05105679 supplier, PF05105679, selective, transient-receptor-potential, TRPM8, ion, channels, blocks, blockers, orally, bioavailable, TRPM, 6003, Tocris Bioscience
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.