Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

PF-05105679

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
PF-05105679
Identifiers
  • 3-({[(1R)-1-(4-fluorophenyl)ethyl]-(quinoline-3-carbonyl)amino}methyl)benzoic acid
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC26H21FN2O3
Molar mass428.463 g·mol−1
3D model (JSmol)
  • 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=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 theTRPM8ion channel, which is the main receptor responsible for the sensation ofcold. It was developed as a potentialanalgesic, and blocks the sensation of cold in both animals and human trials. It also lowerscore body temperature in small mammals, but does not produce this effect in humans in the normal dosage range.[1][2][3]

See also

[edit]

References

[edit]
  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.
TRPA
Activators
Blockers
TRPC
Activators
Blockers
TRPM
Activators
Blockers
TRPML
Activators
Blockers
TRPP
Activators
Blockers
TRPV
Activators
Blockers
Stub icon

Thispharmacology-related article is astub. You can help Wikipedia byadding missing information.

Retrieved from "https://en.wikipedia.org/w/index.php?title=PF-05105679&oldid=1330450283"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2026 Movatter.jp