From Wikipedia, the free encyclopedia
Investigational analgesic drug
PF-05089771
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4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzene-1-sulfonamide
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PubChem
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Formula | C18H12Cl2FN5O3S2 |
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Molar mass | 500.34 g·mol−1 |
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3D model (
JSmol) | |
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C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F
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InChI=1S/C18H12Cl2FN5O3S2/c19-9-1-2-14(10(3-9)11-6-24-25-18(11)22)29-15-5-13(21)16(4-12(15)20)31(27,28)26-17-7-30-8-23-17/h1-8,26H,(H3,22,24,25) Key:ZYSCOUXLBXGGIM-UHFFFAOYSA-N
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PF-05089771 is a selective,
small-molecule
Nav1.7 and
Nav1.8
voltage-gated sodium channel
blocker under development by
Pfizer as a novel
analgesic.
[1]
[2]
[3] As of June 2014, it has completed
phase II
clinical trials for
wisdom tooth removal and
primary erythromelalgia.
[4]
See also
References
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^ McMahon SB, Koltzenburg M,
Tracey I, Turk D (March 2013).
Wall & Melzack's Textbook of Pain. Elsevier Health Sciences. p. 508.
ISBN
978-0702053740.
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^ Martz L (June 2014).
"Nav-i-gating antibodies for pain". SciBX: Science-Business EXchange. 7 (23): 662.
doi:
10.1038/scibx.2014.662.
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^ Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, et al. (6 April 2016).
"Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release". PLOS ONE. 11 (4): e0152405.
Bibcode:
2016PLoSO..1152405A.
doi:
10.1371/journal.pone.0152405.
PMC
4822888.
PMID
27050761.
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^ Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA (August 2014).
"Recent progress in sodium channel modulators for pain". Bioorganic & Medicinal Chemistry Letters. 24 (16): 3690–3699.
doi:
10.1016/j.bmcl.2014.06.038.
PMID
25060923.
External links
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Calcium |
VDCCsTooltip Voltage-dependent calcium channels | |
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Potassium |
VGKCsTooltip Voltage-gated potassium channels | |
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IRKsTooltip Inwardly rectifying potassium channel | |
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KCaTooltip Calcium-activated potassium channel | |
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K2PsTooltip Tandem pore domain potassium channel | |
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Sodium |
VGSCsTooltip Voltage-gated sodium channels | |
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ENaCTooltip Epithelial sodium channel | |
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ASICsTooltip Acid-sensing ion channel | |
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Chloride |
CaCCsTooltip Calcium-activated chloride channel | |
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CFTRTooltip Cystic fibrosis transmembrane conductance regulator | |
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Unsorted | |
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Others |
TRPsTooltip Transient receptor potential channels | |
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LGICsTooltip Ligand gated ion channels | |
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