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PF-05089771 Legal status
US : Investigational New Drug
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 PubChem CID ChemSpider UNII ChEMBL Formula C 18 H 12 Cl 2 F N 5 O 3 S 2 Molar mass 500.34 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-molecule Nav 1.7 and Nav 1.8 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 [ ]
List of investigational analgesics
References [ ]
^ McMahon SB, Koltzenburg M, Tracey I, Turk D (March 2013). Wall & Melzack's Textbook of Pain . Elsevier Health Sciences. p. 508. ISBN 978-0702053740 .
^ Martz L (June 2014). "Nav-i-gating antibodies for pain" . SciBX: Science-Business EXchange . 7 (23): 662. doi :10.1038/scibx.2014.662 .
^ 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 .
^ 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): 3690–9. doi :10.1016/j.bmcl.2014.06.038 . PMID 25060923 .
External links [ ]
Analgesics (N02A , N02B )
Opioids
Opiates /opium
Codeine #
Morphine # (+naltrexone )
Opium
Laudanum
Paregoric
Semisynthetic Synthetic
Paracetamol -typeNSAIDs
Propionates Oxicams
Isoxicam
Lornoxicam
Meloxicam
Piroxicam
Tenoxicam
Acetates COX-2 inhibitors Fenamates Salicylates Pyrazolones
Aminophenazone ‡
Ampyrone
Metamizole (dipyrone)
Nifenazone
Phenazone
Propyphenazone (+paracetamol/caffeine )
Others
Cannabinoids
Cannabidiol
Cannabis
Nabilone
Nabiximols
Tetrahydrocannabinol (dronabinol)
Ion channel modulators
Calcium blockers
Alcohol (ethanol)
Gabapentin
Gabapentin enacarbil
Leconotide
Mirogabalin
Pregabalin
Ziconotide
Sodium blockers
Carbamazepine
Lacosamide
Local anesthetics (e.g., cocaine , lidocaine )
Mexiletine
Nefopam
Tricyclic antidepressants (e.g., amitriptyline # )
Potassium openers
Myorelaxants
Carisoprodol
Chlorzoxazone
Cyclobenzaprine
Mephenoxalone
Methocarbamol
Orphenadrine
Others
# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
Calcium
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hERG (KCNH2, Kv 11.1)-specific: Ajmaline
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BRL-32872
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E-4031
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PNU-282,987
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GAL-021
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12-O-Tetradecanoylphorbol-13-acetate
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Sodium
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Toxins: Conotoxins
Neosaxitoxin
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Others: Buprenorphine
Evenamide
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Safinamide
Tricyclic antidepressants
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ENaC
Blockers
Amiloride
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Blockers
Amiloride
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See also: Receptor/signaling modulators • Transient receptor potential channel modulators
Categories :
Analgesics Sodium channel blockers Fluoroarenes Chlorobenzenes Thiadiazoles Pyrazoles Sulfonamides Analgesic stubs Hidden categories:
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