PF-05105679

PF-05105679
Identifiers
	IUPAC name 3-({[(1R)-1-(4-fluorophenyl)ethyl]-(quinoline-3-carbonyl)amino}methyl)benzoic acid;
CAS Number	1398583-31-7;
PubChem CID	60195662;
DrugBank	DB15450;
ChemSpider	57871141;
UNII	F2B10OFV7Y;
ChEMBL	ChEMBL3577885;
CompTox Dashboard (EPA)	DTXSID301336742 ;
Chemical and physical data
Formula	C26H21FN2O3
Molar mass	428.463 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@H](C1=CC=C(C=C1)F)N(CC2=CC(=CC=C2)C(=O)O)C(=O)C3=CC4=CC=CC=C4N=C3;
	InChI InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1; Key:BXNMZRPTQFVRFA-QGZVFWFLSA-N;

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]

References

^ Winchester WJ, Gore K, Glatt S, Petit W, Gardiner JC, Conlon K, et al. (November 2014). "Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans". The Journal of Pharmacology and Experimental Therapeutics. 351 (2): 259–69. doi:10.1124/jpet.114.216010. PMID 25125580. S2CID 19407401.
^ Andrews MD, Af Forselles K, Beaumont K, Galan SR, Glossop PA, Grenie M, et al. (April 2015). "Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain". ACS Medicinal Chemistry Letters. 6 (4): 419–24. doi:10.1021/ml500479v. PMC 4394344. PMID 25893043.
^ Gosset JR, Beaumont K, Matsuura T, Winchester W, Attkins N, Glatt S, et al. (November 2017). "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. doi:10.1016/j.ejps.2017.06.009. PMID 28603038. S2CID 28787846.

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[1] Winchester WJ, Gore K, Glatt S, Petit W, Gardiner JC, Conlon K, et al. (November 2014). "Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans". The Journal of Pharmacology and Experimental Therapeutics. 351 (2): 259–69. doi:10.1124/jpet.114.216010. PMID 25125580. S2CID 19407401.

[2] Andrews MD, Af Forselles K, Beaumont K, Galan SR, Glossop PA, Grenie M, et al. (April 2015). "Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain". ACS Medicinal Chemistry Letters. 6 (4): 419–24. doi:10.1021/ml500479v. PMC 4394344. PMID 25893043.

[3] Gosset JR, Beaumont K, Matsuura T, Winchester W, Attkins N, Glatt S, et al. (November 2017). "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. doi:10.1016/j.ejps.2017.06.009. PMID 28603038. S2CID 28787846.

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See also

References