PF-05105679 explained
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
Notes and References
- Winchester WJ, Gore K, Glatt S, Petit W, Gardiner JC, Conlon K, Postlethwaite M, Saintot PP, Roberts S, Gosset JR, Matsuura T, Andrews MD, Glossop PA, Palmer MJ, Clear N, Collins S, Beaumont K, Reynolds DS . 6 . 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 . 25125580 . 10.1124/jpet.114.216010 . 19407401 . free .
- Andrews MD, Af Forselles K, Beaumont K, Galan SR, Glossop PA, Grenie M, Jessiman A, Kenyon AS, Lunn G, Maw G, Owen RM, Pryde DC, Roberts D, Tran TD . 6 . Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain . ACS Medicinal Chemistry Letters . 6 . 4 . 419–24 . April 2015 . 25893043 . 10.1021/ml500479v . 4394344 .
- Gosset JR, Beaumont K, Matsuura T, Winchester W, Attkins N, Glatt S, Lightbown I, Ulrich K, Roberts S, Harris J, Mesic E, van Steeg T, Hijdra D, van der Graaf PH . 6 . 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 . 28603038 . 10.1016/j.ejps.2017.06.009 . 28787846 .
