PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC
50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonist, PF-05105679 [(
R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid] acts as a clinical tool to assess the function of TRPM8 in modulating the body temperature. It also helps to determine its role in the treatment of pain in humans.
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