PF-05089771

Investigational analgesic drug
  • US: Investigational New Drug
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
  • 1235403-62-9
PubChem CID
  • 46840946
ChemSpider
  • 29411106
UNII
  • 25U4N985O2
ChEMBL
  • ChEMBL2325014
Chemical and physical dataFormulaC18H12Cl2FN5O3S2Molar mass500.34 g·mol−13D model (JSmol)
  • Interactive image
  • C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F
InChI
  • 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-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

  1. ^ McMahon SB, Koltzenburg M, Tracey I, Turk D (March 2013). Wall & Melzack's Textbook of Pain. Elsevier Health Sciences. p. 508. ISBN 978-0702053740.
  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

  • "PF-05089771". AdisInsight. Springer Nature Switzerland AG.
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Opioids
Opiates/opium
Semisynthetic
Synthetic
Paracetamol-typeNSAIDs
Propionates
Oxicams
Acetates
COX-2 inhibitors
Fenamates
Salicylates
Pyrazolones
Others
CannabinoidsIon channel
modulators
Calcium blockers
Sodium blockers
Potassium openers
MyorelaxantsOthers
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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
  • GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
KCaTooltip Calcium-activated potassium channel
Blockers
  • BKCa-specific: Ethanol (alcohol)
  • GAL-021
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
  • Solnatide
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
  • See here instead.
LGICsTooltip Ligand gated ion channels
  • See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators


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