A novel selective and orally bioavailable Nav1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability

British Journal of Pharmacology

Volumn 172, Issue 10, 2015, Pages 2654-2670

  Payne, Claire Elizabeth ^a   Brown, Adam R ^a   Theile, Jonathon W ^b   Loucif, Alexandre J C ^a   Alexandrou, Aristos J ^a   Fuller, Mathew D ^b   Mahoney, John H ^b   Antonio, Brett M ^b   Gerlach, Aaron C ^b   Printzenhoff, David M ^b   Prime, Rebecca L ^a   Stockbridge, Gillian ^a   Kirkup, Anthony J ^a   Bannon, Anthony W ^b   England, Steve ^a   Chapman, Mark L ^b   Bagal, Sharan ^a   Roeloffs, Rosemarie ^b   Anand, Uma ^c   Anand, Praveen ^c   Bungay, Peter J ^a   Kemp, Mark ^a   Butt, Richard P ^a   Stevens, Edward B ^a   more..

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b PFIZER INC   (United States)

^c HAMMERSMITH HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

6 AMINO 5 (2,3,5 TRICHLORO PHENYL)PYRIDINE 2 CARBOXYLIC ACID METHYLAMIDE; SODIUM CHANNEL BLOCKING AGENT; SODIUM CHANNEL NAV1.8; UNCLASSIFIED DRUG; 6-AMINO-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE; PICOLINIC ACID DERIVATIVE; SCN10A PROTEIN, HUMAN; TETRODOTOXIN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; ATTENUATION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG POTENCY; DRUG STRUCTURE; HUMAN; HUMAN CELL; IC50; IN VIVO STUDY; INFLAMMATORY PAIN; MALE; MOUSE; NERVE CELL EXCITABILITY; NERVE POTENTIAL; NEUROPATHIC PAIN; NOCICEPTION; NONHUMAN; PRIORITY JOURNAL; RAT; SITE DIRECTED MUTAGENESIS; SPINAL GANGLION; STEADY STATE; ACTION POTENTIAL; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; HEK293 CELL LINE; MEMBRANE POTENTIAL; ORAL DRUG ADMINISTRATION; PAIN MEASUREMENT; SENSORY NERVE CELL;

ACTION POTENTIALS; ADMINISTRATION, ORAL; ANIMALS; GANGLIA, SPINAL; HEK293 CELLS; HUMANS; MEMBRANE POTENTIALS; NAV1.8 VOLTAGE-GATED SODIUM CHANNEL; NOCICEPTION; PAIN MEASUREMENT; PICOLINIC ACIDS; RATS; SENSORY RECEPTOR CELLS; SODIUM CHANNEL BLOCKERS; TETRODOTOXIN;

EID: 84928325520     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.13092     Document Type: Article

References (50)

1. Abrahamsen B, Zhao J, Asante CO, Cendan CM, Marsh S, Martinez-Barbera JP, et al. (2008). The cell and molecular basis of mechanical, cold, and inflammatory pain. Science 321: 702-705.
2. Akopian AN, Souslova V, England S, Okuse K, Ogata N, Ure J, et al. (1999). The tetrodotoxin-resistant sodium channel SNS has a specialized function in pain pathways. Nat Neurosci 2: 541-548.
3. Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Catterall WA, et al. (2013). The Concise Guide to PHARMACOLOGY 2013/14: Ion Channels. Br J Pharmacol 170: 1607-1651.
4. Amaya F, Decosterd I, Samad T, Plumpton C, Tate S, et al. (2000). Diversity of expression of the sensory neuron-specific TTX-resistant voltage-gated sodium ion channels SNS and SNS2. Mol Cell Neurosci 15: 331-342.
5. Anand U, Otto WR, Casula MA, Day NC, Davis JB, Bountra C, et al. (2006). The effect of neurotrophic factors on morphology, TRPV1 expression and capsaicin responses of cultured human DRG sensory neurons. Neurosci Lett 399: 51-56.
6. Black JA, Nikolajsen L, Kroner K, Jensen TS, Waxman SG, (2008). Multiple sodium channel isoforms and mitogen-activated protein kinases are present in painful human neuromas. Ann Neurol 64: 644-653.
7. 2+ current in the action potentials of nociceptive sensory neurons. J Neurosci 22: 10277-10290.
8. van den Boogaard M, Smemo S, Burnicka-Turek O, Arnolds TE, van de Werken HJ, Klaus P, et al. (2014). A common genetic variant within SCN10A modulates cardiac SCN5A expression. J Clin Invest 124: 1844-1852.
9. Browne LE, Blaney FE, Yusaf SP, Clare JJ, Wray D, (2009). Structural determinants of drugs acting on the Nav1.8 channel. J Biol Chem 284: 10523-10536.
10. Castle N, Printzenhoff D, Zellmer S, Antonio B, Wickenden A, Silvia C, (2009). Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platforms. Comb Chem High Throughput Screen 12: 107-122.
11. Chambers JC, Zhao J, Terracciano CM, Bezzina CR, Zhang W, Kaba R, et al. (2010). Genetic variation in SCN10A influences cardiac conduction. Nat Genet 42: 149-152.
12. Chaplan SR, Bach FW, Pogrel JW, Chung JM, Yaksh TL, (1994). Quantitative assessment of tactile allodynia in the rat paw. J Neurosci Methods 53: 55-63.
13. Coggeshall RE, Tate S, Carlton SM, (2004). Differential expression of tetrodotoxin-resistant sodium channels Nav1.8 and Nav1.9 in normal and inflamed rats. Neurosci Lett 355: 45-48.
14. Coward K, Plumpton C, Facer P, Birch R, Carlstedt T, Tate S, et al. (2000). Immunolocalization of SNS/PN3 and NaN/SNS2 sodium channels in human pain states. Pain 85: 41-50.
15. Cummins TR, Sheets PL, Waxman SG, (2007). The roles of sodium channels in nociception: implications for mechanisms of pain. Pain 131: 243-257.
16. Dib-Hajj SD, Black JA, Waxman SG, (2009). Voltage gated sodium channels: therapeutic targets for pain. Pain Med 10: 1260-1269.
17. Dib-Hajj SD, Cummins TR, Black JA, Waxman SG, (2010). Sodium channels in normal and pathological pain. Annu Rev Neurosci 33: 325-347.
18. Djouhri L, Fang X, Okuse K, Wood JN, Berry CM, Lawson SN, (2003). The TTX-resistant sodium channel Nav1.8 (SNS/PN3): expression and correlation with membrane properties in rat nociceptive primary afferent neurons. J Physiol 550: 739-752.
19. V1.8 tetrodotoxin-resistant sodium channel reverses mechanical allodynia in neuropathic rats. Neuroscience 146: 812-821.
20. England S, de Groot MJ, (2009). Subtype selective targeting of voltage-gated sodium channels. Br J Pharmacol 158: 1413-1425.
21. England S, Bevan S, Docherty RJ, (1996). PGE2 modulates the tetrodotoxin-resistant sodium current in neonatal rat dorsal root ganglion neurones via the cyclic AMP-protein kinase A cascade. J Physiol 495: 429-440.
22. Faber CG, Lauria G, Merkies IS, Cheng X, Han C, Ahn HS, et al. (2012). Gain-of-function Nav1.8 mutations in painful neuropathy. Proc Natl Acad Sci U S A 109: 19444-19449.
23. Fjell J, Cummins TR, Dib-Hajj SD, Fried K, Black JA, Waxman SG, (1999). Differential role of GDNF and NGF in the maintenance of two TTX-resistant sodium channels in adult DRG neurons. Brain Res Mol Brain Res 67: 267-282.
24. Gerner P, Strichartz GR, (2008). Sensory and motor complications of local anaesthetics. Muscle Nerve 37: 421-425.
25. V1.8 mutation in small fibre neuropathy: impaired inactivation underlying DRG neuron hyperexcitability. J Neurol Neurosurg Psychiatry 85: 499-505.
26. V1.8 mutation shifts activation to hyperpolarised potentials and increases excitability of dorsal root ganglion neurons. J Neurosci 33: 14087-14097.
27. Jackson AL, Linsley PS, (2010). Recognizing and avoiding siRNA off-target effects for target identification and therapeutic application. Nat Rev Drug Discov 9: 57-67.
28. Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, et al. (2007). A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci USA 104: 8520-8525.
29. Kerr BJ, Souslova V, McMahon SB, Wood JN, (2001). A role for the TTX-resistant sodium channel Nav1.8 in NGF-induced hyperalgesia, but not neuropathic pain. Neuroreport 12: 3077-3080.
30. Khasar SG, Gold MS, Levine JD, (1998). A tetrodotoxin-resistant sodium channel mediates inflammatory pain in the rat. Neurosci Lett 256: 17-20.
31. Kilkenny C, Browne W, Cuthill IC, Emerson M, Altman DG, Group NCRRGW (2010). Animal research: reporting in vivo experiments: the ARRIVE guidelines. Br J Pharmacol 160: 1577-1579.
32. Kim SH, Chung JM, (1992). An experimental model for peripheral neuropathy produced by segmental spinal nerve ligation in the rat. Pain 50: 355-363.
33. Lane CAL, Maw GN, Rawson DJ, Thompson LR, (2006). Pyridine derivatives. PCT Int. Appl. WO 2006011050.
34. McGrath JC, Drummond GB, McLachlan EM, Kilkenny C, Wainwright CL, (2010). Guidelines for reporting experiments involving animals: the ARRIVE guidelines. Br J Pharmacol 160: 1573-1576.
35. Minett MS, Falk S, Santana-Varela S, Bogdanov YD, Nassar MA, Heegaard AM, et al. (2014). Pain without nociceptors? Nav1.7-independent pain mechanisms. Cell Rep 6: 301-312.
36. Moser VC, (1992). Applications of a neurobehavioural screening battery. J Am Coll Toxicol 10: 661-669.
37. Nassar MA, Levato A, Stirling LC, Wood JN, (2005). Neuropathic pain develops normally in mice lacking both Na(v)1.7 and Na(v)1.8. Mol Pain 22: 1-24.
38. Passmore GM, (2005). Dorsal root ganglion neurones in culture: a model for identifying novel analgesic targets. J Pharmacol Toxicol Methods 51: 201-208.
39. Pawson AJ, Sharman JL, Benson HE, Faccenda E, Alexander SP, Buneman OP, et al.; NC-IUPHAR (2014). The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledge base of drug targets and their ligands. Nucl Acids Res 42 (Database Issue): D1098-D1106.
40. V1.8 sodium channels to action potential electrogenesis in DRG neurons. J Neurophysiol 86: 629-640.
41. Renton T, Yiangou Y, Plumpton C, Tate S, Bountra C, Anand P, (2005). Sodium channel Nav1.8 immunoreactivity in painful human dental pulp. BMC Oral Health 5: 5.
42. V1.8 is essential for the expression of spontaneous activity in damaged sensory axons of mice. J Physiol 550: 921-926.
43. V1.8) mRNA accumulation to sciatic nerve injury-induced painful neuropathy in rats. J Biol Chem 286: 39836-39847.
44. V1.8 sodium channels. Mol Interv 7: 192-195.
45. Shields SD, Ahn HS, Yang Y, Han C, Seal RP, Wood JN, et al. (2012). Nav1.8 expression is not restricted to nociceptors in mouse peripheral nervous system. Pain 153: 2017-2030.
46. Sindrup SH, Jensen TS, (2007). Are sodium channel blockers useless in peripheral neuropathic pain? Pain 128: 6-7.
47. V1.8 mRNA up-regulation in painful neuropathy. Mol Pain 5: 14.
48. V1.8 sodium channel in the maintenance of chronic inflammatory hypernociception. Neurosci Lett 386: 72-77.
49. Yaksh TL, Ozaki G, McCumber D, Rathbun M, Svensson C, Malkmus S, et al. (2001). An automated flinch detecting system for use in the formalin nociceptive bioassay. J Appl Physiol 90: 2386-2402.
50. V1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats. Neuropharmacology 59: 201-207.