Chemistry:PF-05105679

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Short description: Chemical compound
PF-05105679
PF-05105679 structure.png
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC26H21FN2O3
Molar mass428.463 g·mol−1
3D model (JSmol)

PF-05105679 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold. It was developed as a potential analgesic, and blocks the sensation of cold in both animals and human trials. It also lowers core body temperature in small mammals, but does not produce this effect in humans in the normal dosage range.[1][2][3]

See also

References

  1. "Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans". The Journal of Pharmacology and Experimental Therapeutics 351 (2): 259–69. November 2014. doi:10.1124/jpet.114.216010. PMID 25125580. 
  2. "Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain". ACS Medicinal Chemistry Letters 6 (4): 419–24. April 2015. doi:10.1021/ml500479v. PMID 25893043. 
  3. "A cross-species translational pharmacokinetic-pharmacodynamic evaluation of core body temperature reduction by the TRPM8 blocker PF-05105679". European Journal of Pharmaceutical Sciences 109S: S161–S167. November 2017. doi:10.1016/j.ejps.2017.06.009. PMID 28603038.