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PF-05089771

From Wikipedia, the free encyclopedia
Investigational analgesic drug
Pharmaceutical compound
PF-05089771
Legal status
Legal status
Identifiers
  • 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzene-1-sulfonamide
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H12Cl2FN5O3S2
Molar mass500.34 g·mol−1
3D model (JSmol)
  • C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F
  • 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

PF-05089771 is a selective,small-moleculeNav1.7 andNav1.8voltage-gated sodium channelblocker under development byPfizer as a novelanalgesic.[1][2][3] As of June 2014, it has completedphase IIclinical trials forwisdom tooth removal andprimary erythromelalgia.[4]

See also

[edit]

References

[edit]
  1. ^McMahon SB, Koltzenburg M,Tracey I, Turk D (March 2013).Wall & Melzack's Textbook of Pain. Elsevier Health Sciences. p. 508.ISBN 978-0-7020-5374-0.
  2. ^Martz L (June 2014)."Nav-i-gating antibodies for pain".SciBX: Science-Business EXchange.7 (23): 662.doi:10.1038/scibx.2014.662.
  3. ^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.
  4. ^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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Opioids
Opiates/opium
Semisynthetic
Synthetic
Paracetamol-type
NSAIDs
Propionates
Oxicams
Acetates
COX-2 inhibitors
Fenamates
Salicylates
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Cannabinoids
Ion channel
modulators
Calcium blockers
Sodium blockers
Potassium openers
Myorelaxants
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Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
KCaTooltip Calcium-activated potassium channel
Blockers
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
LGICsTooltip Ligand gated ion channels


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