Neuronal nicotinic receptors as targets for novel analgesics

Expert Opinion on Investigational Drugs

Volumn 14, Issue 10, 2005, Pages 1191-1198

  Vincler, Michelle ^a  

^a WAKE FOREST SCHOOL OF MEDICINE   (United States)

Author keywords

A 85380; ABT 594; Choline; Chronic pain; Epibatidine; Macrophage; Microglia; Nerve injury; Neuroinflammation; Neuroprotection

Indexed keywords

2ALPHA (2 CHLOROPYRIDINYL)AZABICYCLO[3.2.1]OCTANE; 2BETA (2 CHLOROPYRIDINYL)AZABICYCLO[3.2.1]OCTANE; 3 (2 AZETIDINYLMETHOXY)PYRIDINE; 5 (2 AZETIDINYLMETHOXY) 2 CHLOROPYRIDINE; A 36683; A 366833; ACETYLSALICYLIC ACID; ANALGESIC AGENT; ANTINOCICEPTIVE AGENT; CHOLINE; CLONIDINE; EPIBATIDINE; EPIBOXIDINE; HOMOEPIBOXIDINE; METANICOTINE; MORPHINE; NEOSTIGMINE; NEUROPROTECTIVE AGENT; NEW DRUG; NICOTINE; NICOTINIC AGENT; NICOTINIC RECEPTOR; NONSTEROID ANTIINFLAMMATORY AGENT; OPIATE AGONIST; UNCLASSIFIED DRUG;

ANALGESIA; ANTIINFLAMMATORY ACTIVITY; ANTINOCICEPTION; ATTENUATION; CENTRAL NERVOUS SYSTEM; CHOLINERGIC TRANSMISSION; CHRONIC INFLAMMATION; CHRONIC PAIN; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG SAFETY; DRUG TARGETING; DRUG USE; HUMAN; HYPERALGESIA; IMMUNE RESPONSE; NEUROPATHIC PAIN; NEUROPROTECTION; NONHUMAN; PATHOPHYSIOLOGY; PERIPHERAL NERVE INJURY; PERIPHERAL NERVOUS SYSTEM; PROTEIN EXPRESSION; REVIEW; SPINAL CORD INJURY;

ANALGESICS; ANIMALS; HUMANS; NEURONS; NICOTINIC AGONISTS; PAIN; RECEPTORS, NICOTINIC;

EID: 27144493036     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.14.10.1191     Document Type: Review

References (87)

1. GOTTI C, CLEMENTI F: Neuronal nicotinic receptors: from structure to pathology. Prog. Neurobiol. (2004) 74(6):363-396.
2. 3 nicotinic receptors. J. Pharmacol. Exp. Ther. (1998) 286(1):311-320.
3. 4 neuronal nicotinic receptors. J. Biol. Chem. (2003) 278(45):44033-44040.
4. 5 subunits. J. Physiol. (1999) 516(3)657-678.
5. LUKAS RJ, CHANGEUX JP, LE NOVERE N et al.: International Union of Pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits. Pharmacol. Rev. (1999) 51(2):397-401.
6. COLQUHOUN LM, PATRICK JW: Pharmacology of neuronal nicotinic acetylcholine receptor subtypes. Adv. Pharmacol. (1997) 39:191-220.
7. CORDERO-ERAUSQUIN M, PONS S, FAURE P, CHANGEUX JP: Nicotine differentially activates inhibitory and excitatory neurons in the dorsal spinal cord. Pain (2004) 109(3):308-318.
8. HABERBERGER RV, BERNARDINI N, KRESS M et al.: Nicotinic acetylcholine receptor subtypes in nociceptive dorsal root ganglion neurons of the adult rat. Auton. Neurosci. (2004) 113(1-2):32-42.
9. LÉNA C, DE KERCHOVE D'E, CORDERO-ERAUSQUIN M et al.: Diversity and distribution of nicotinic acetylcholine receptors in the locus ceruleas neurons. Proc. Natl. Acad. Sci. USA (1999) 96(21):12126-12131.
10. KHAN I, OSAKA H, STANISLAUS S et al.: Nicotinic acetylcholine receptor distribution in relation to spinal neurotransmission pathways. J. Comp. Neurol. (2003) 467(1):44-59.
11. GENZEN JR, McGEHEE DS: Short- and long-term enhancement of excitatory transmission in the spinal cord dorsal horn by nicotinic acetylcholine receptors. Proc. Natl. Acad. Sci. USA (2003) 100(11):6807-6812.
12. MIAO FJ, GREEN PG, BENOWITZ N, LEVINE JD: Central terminals of nociceptors are targets for nicotine suppression of inflammation. Neuroscience (2004) 123(3):777-784.
13. ROBERTS RG, STEVENSON JE, WESTERMAN RA, PENNEFATHER J: Nicotinic acetylcholine receptors on capsaicin-sensitive nerves. Neuroreport (1995) 6(11):1578-1582.
14. KHAN IM, WENNERHOLM M, SINGLETARY E et al.: Ablation of primary afferent terminals reduces nicotinic receptor expression and the nociceptive responses to nicotinic agonists in the spinal cord. J. Neurocytol. (2004) 33(5):543-556.
15. LI X, RAINNIE DG, McCARLEY RW, GREENE RW: Presynaptic nicotinic receptors facilitate monoaminergic transmission. J. Neurosci. (1998) 18(5):1904-1912.
16. GENZEN JR, McGEHEE DS: Nicotinic modulation of GABAergic synaptic transmission in the spinal cord dorsal horn. Brain Res. (2005) 1031(2):229-237.
17. PLENGE P, MELLERUP ET, WORTWEIN G: Characterization of epibatidine binding to medial habenula: potential role in analgesia. J. Pharmacol. Exp. Ther. (2002) 302(2):759-765.
18. CORDERO-ERAUSQUIN M, CHANGEUX JP: Tonic nicotinic modulation of serotoninergic transmission in the spinal cord. Proc. Natl. Acad. Sci. USA (2001) 98(5):2803-2807.
19. LI X, PAN HL, XU Z, TOBIN JR, EISENACH JC: Nicotinic cholinergic receptor mediates norepinephrine release in rat spinal cord: an in vivo microdialysis study. Society for Neuroscience (2000):356.9 (Abstract).
20. LI X, EISENACH JC: Nicotinic acetylcholine receptor regulation of spinal norepinephrine release. Anesthesiology (2002) 96(6):1450-1456.
21. VILLERS-THIERY A, BOURGEOIS JP, PONS S et al.: An in vitro study of the subcellular distribution of nicotinic receptors. Biol. Cell (2003) 95(6):373-381.
22. 7-Containing nicotinic receptors are segregated to the somatodendritic membrane of the cholinergic neurons in the avian nucleus semilunaris. Neuroscience (2001) 103(2):541-550.
23. VERNALLIS AB, CONROY WG, BERG DK: Neurons assemble acetylcholine receptors with as many as three kinds of subunits while maintaining subunit segregation among receptor subtypes. Neuron (1993) 10(3):451-464.
24. IWAMOTO ET, MARION L: Adrenergic, serotonergic and cholinergic components of nicotinic antinociception in rats. J. Pharmacol. Ex. Ther. (1993) 265(2):777-789.
25. MARUBIO LM, MAR ARROYO-JIMENEZ M, CORDERO-ERAUSQUIN M et al.: Reduced antinociception in mice lacking neuronal nicotinic receptor subunits. Nature (1999) 398(6730):805-810.
26. DECKER MW, MEYER MD, SULLIVAN JP: The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin. Invest. Drugs (2001) 10(10):1819-1830.
27. NISHIYAMA T, GYERMEK L, TRUDELL ML, HANAOKA K: Spinally mediated analgesia and receptor binding affinity of epibatidine analogs. Eur. J. Pharmacol. (2003) 470(1-2):27-31.
28. FITCH RW, PEI XF, KANEKO Y et al.: Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg. Med. Chem. (2004) 12(1):179-190.
29. KESINGLAND AC, GENTRY CT, PANESAR MS et al.: Analgesic profile of the nicotinic acetylcholine receptor agonists, (+)-epibatidine and ABT-594 in models of persistent inflammatory and neuropathic pain. Pain (2000) 86(1-2):113-118.
30. KHAN IM, BUERKLE H, TAYLOR P, YAKSH TL: Nociceptive and antinociceptive responses to intrathecally administered nicotinic agonists. Neuropharmacology (1998) 37(12):1515-1525.
31. RASHID MH, UEDA H: Neuropathy-specific analgesic action of intrathecal nicotinic agonists and its spinal GABA-mediated mechanism. Brain Res. (2002) 953(1-2):53-62.
32. CURZON P, NIKKEL AL, BANNON AW, ARNERIC SP, DECKER MW: Differences between the antinociceptive effects of the cholinergic channel activators A-85380 and (±)-epibatidine in rats. J. Pharmacol. Exp. Ther. (1998) 287(3):847-853.
33. RUETER LE, KOHLHAAS KL, CURZON P, SUROWY CS, MEYER MD: Peripheral and central sites of action for A-85380 in the spinal nerve ligation model of neuropathic pain. Pain (2003) 103(3):269-276.
34. BUNNELLE, WILLIAM H: Development of neuronal nicotinic receptor (NNR) agonists as novel analgesics. The 228th ACS National Meeting, Philadelphia, USA (2004).
35. LYNCH JJ III, WADE CL, MIKUSA JP, DECKER MW, HONORE P: ABT-594 (a nicotinic acetylcholine agonist): anti-allodynia in a rat chemotherapy-induced pain model. Eur. J. Pharmacol. (2005) 509(1):43-48.
36. WANG Y, SU DM, WANG RH, LIU Y, WANG H: Antinociceptive effects of choline against acute and inflammatory pain. Neuroscience (2005) 132(1):49-56.
37. HAMA AT, LLOYD GK, MENZAGHI F: The antinociceptive effect of intrathecal administration of epibatidine with clonidine or neostigmine in the formalin test in rats. Pain (2001) 91(1-2):131-138.
38. ZARRINDAST MR, PAZOUKI M, NASSIRI-RAD S: Involvement of cholinergic and opioid receptor mechanisms in nicotine-induced antinociception. Pharmacol. Toxicol. (1997) 81(5):209-213.
39. FLOOD P, DANIEL D: Intranasal nicotine for postoperative pain treatment. Anesthesiology (2004) 101(6):1417-1421.
40. ZIMMERMANN M: Pathobiology of neuropathic pain. Eur. J. Pharmacol. (2001) 429(1-3):23-37.
41. JI RR, WOOLF CJ: Neuronal plasticity and signal transduction in nociceptive neurons: implications for the initiation and maintenance of pathological pain. Neurobiol. Dis. (2001) 8(1):1-10.
42. VALDER CR, LIU JJ, SONG YH, LUO ZD: Coupling gene chip analyses and rat genetic variances in identifying potential target genes that may contribute to neuropathic allodynia development. J. Neurochem. (2003) 87(3):560-573.
43. XIAO HS, HUANG QH, ZHANG FX et al.: Identification of gene expression profile of dorsal root ganglion in the rat peripheral axotomy model of neuropathic pain. Proc. Natl. Acad. Sci. USA (2002) 99(12):8360-8365.
44. YANG L, ZHANG FX, HUANG F et al.: Peripheral nerve injury induces transsynaptic modification of channels, receptors and signal pathways in rat dorsal spinal cord. Eur. J. Neurosci. (2004) 19(4):871-883.
45. VINCLER M, EISENACH JC: Plasticity of spinal nicotinic acetylcholine receptors following spinal nerve ligation. Neurosci. Res. (2004) 48(2):139-145.
46. DUBE GR, KOHLHAAS KL, RUETER LE et al.: Loss of functional neuronal nicotinic receptors in dorsal root ganglion neurons in a rat model of neuropathic pain. Neurosci. Lett. (2005) 376(1):29-34.
47. GILLBERG PG, WIKSTEN B: Effects of spinal cord lesions and rhizotomies on cholinergic and opiate receptor binding sites in rat spinal cord. Acta Physiol. Scand. (1986) 126(4):575-582.
48. GOFF JR, BURKEY AR, GOFF DJ, JASMIN L: Reorganization of the spinal dorsal horn in models of chronic pain: correlation with behaviour. Neuroscience (1998) 82(2):559-574.
49. 2C adrenergic receptor immunoreactivity in the rat spinal cord. Neuroscience (1999) 93 (4):1399-1407.
50. KOHNO T, MOORE KA, BABA H, WOOLF CJ: Peripheral nerve injury alters excitatory synaptic transmission in lamina II of the rat dorsal horn. J. Physiol. (2003) 548(Part 1):131-138.
51. MOORE KA, KOHNO T, KARCHEWSKI LA et al.: Partial peripheral nerve injury promotes a selective loss of GABAergic inhibition in the superficial dorsal horn of the spinal cord. J. Neurosci. (2002) 22(15):6724-6731.
52. WOOLF CJ, SHORTLAND P, COGGESHALL RE: Peripheral nerve injury triggers central sprouting of myelinated afferents. Nature (1992) 355(6355):75-78.
53. KHAN IM, MARSALA M, PRINTZ MP, TAYLOR P, YAKSH TL: Intrathecal nicotinic agonist-elicited release of excitatory amino acids as measured by in vivo spinal microdialysis in rats. J. Pharmacol. Exp. Ther. (1996) 278(1):97-106.
54. GENZEN JR, VAN CLEVE W, McGEHEE DS: Dorsal root ganglion neurons express multiple nicotinic acetylcholine receptor subtypes. J. Neurophysiol. (2001) 86(4):1773-1782.
55. RAU KK, JOHNSON RD, COOPER BY: Nicotinic AChR in subclassified capsaicin sensitive and insensitive nociceptors of the rat DRG. J. Neurophysiol. (2004) 93(3):1358-1371.
56. WATKINS LR, MILLIGAN ED, MAIER SF: Glial activation: a driving force for pathological pain. Trends Neurosci. (2001) 24(8):450-455.
57. BENDSZUS M, STOLL G: Caught in the act: in vivo mapping of macrophage infiltration in nerve injury by magnetic resonance imaging. J. Neurosci. (2003) 23(34):10892-10896.
58. HU P, McLACHLAN EM: Distinct functional types of macrophage in dorsal root ganglia and spinal nerves proximal to sciatic and spinal nerve transections in the rat. Exp. Neurol. (2003) 184(2):590-605.
59. MUELLER M, LEONHARD C, WACKER K et al.: Macrophage response to peripheral nerve injury: the quantitative contribution of resident and hematogenous macrophages. Lab. Invest. (2003) 83(2):175-185.
60. STUESSE SL, CRUCE WL, LOVELL JA, McBURNEY DL, CRISP T: Microglial proliferation in the spinal cord of aged rats with a sciatic nerve injury. Neurosci. Lett. (2000) 287(2):121-124.
61. GAZDA LS, MILLIGAN ED, HANSEN MK et al.: Sciatic inflammatory neuritis (SIN): behavioral allodynia is paralleled by peri-sciatic proinflammatory cytokine and superoxide production. J. Peripher. Nerv. Syst. (2001) 6(3):111-129.
62. RAGHAVENDRA V, TANGA F, DELEO JA: Inhibition of microglial activation attenuates the development but not existing hypersensitivity in a rat model of neuropathy. J. Pharmacol. Exp. Ther. (2003) 306(2):624-630.
63. WANG H, YU M, OCHANI M et al.: Nicotinic acetylcholine receptor alpha7 subunit is an essential regulator of inflammation. Nature (2003) 421(6921):384-388.
64. 2 in rat microglial cultures. J. Neuroinflam. (2005) 2(1):4.
65. 4 nicotinic receptor agonist, epibatidine. J. Pharmacol. Exp. Ther. (2004) 313(1):389-394.
66. DAMAJ MI, GLASSCO W, ACETO MD, MARTIN BR: Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. J. Pharmacol. Exp. Ther. (1999) 291(1):390-398.
67. GILBERT SD, CLARK TM, FLORES CM: Antihyperalgesic activity of epibatidine in the formalin model of facial pain. Pain (2001) 89(2-3):159-165.
68. LAWAND NB, LU Y, WESTLUND KN: Nicotinic cholinergic receptors: potential targets for inflammatory pain relief. Pain (1999) 80(1-2):291-299.
69. KALRA R, SINGH SP, PENA-PHILIPPIDES JC et al.: Immunosuppressive and anti-inflammatory effects of nicotine administered by patch in an animal model. Clin. Diagn. Lab. Immunol. (2004) 11(3):563-568.
70. 7 nicotinic receptors. J. Neurochem. (2004) 89(2):337-343.
71. NAKAYAMA H, NUMAKAWA T, IKEUCHI T, HATANAKA H: Nicotine-induced phosphorylation of extracellular signal-regulated protein kinase and CREB in PC12h cells. J. Neurochem. (2001) 79(3):489-498.
72. JI RR, BABA H, BRENNER GJ, WOOLF CJ: Nociceptive-specific activation of ERK in spinal neurons contributes to pain hypersensitivity. Nat. Neurosci. (1999) 2(12):1114-1119.
73. OBATA K, YAMANAKA H, DAI Y et al.: Differential activation of MAPK in injured and uninjured DRG neurons following chronic constriction injury of the sciatic nerve in rats. Eur. J. Neurosci. (2004) 20(11):2881-2895.
74. TRACEY KJ: The inflammatory reflex. Nature (2002) 420(6917):853-859.
75. DECKER MW, MEYER MD: Therapeutic potential of neuronal nicotinic acetylcholine receptor agonists as novel analgesics. Biochem. Pharmacol. (1999) 58(6):917-923.
76. MILLIGAN ED, TWINING C, CHACUR M et al.: Spinal glia and proinflammatory cytokines mediate mirror-image neuropathic pain in rats. J. Neurosci. (2003) 23(3):1026-1040.
77. WIESELER-FRANK J, MAIER SF, WATKINS LR: Glial activation and pathological pain. Neurochem. Int. (2004) 45(2-3):389-395.
78. SIDDALL PJ, McCLELLAND JM, RUTKOWSKI SB, COUSINS MJ: A longitudinal study of the prevalence and characteristics of pain in the first 5 years following spinal cord injury. Pain (2003) 103(3):249-257.
79. PROFYRIS C, CHEEMA SS, ZANG D et al.: Degenerative and regenerative mechanisms governing spinal cord injury. Neurobiol. Dis. (2004) 15(3):415-436.
80. LIU XZ, XU XM, HU R et al.: Neuronal and glial apoptosis after traumatic spinal cord injury. J. Neurosci. (1997) 17(14):5395-5406.
81. DREW GM, SIDDALL PJ, DUGGAN AW: Mechanical allodynia following contusion injury of the rat spinal cord is associated with loss of GABAergic inhibition in the dorsal horn. Pain (2004) 109(3):379-388.
82. PICCIOTTO MR, ZOLI M: Nicotinic receptors in aging and dementia. J. Neurobiol. (2002) 53(4):641-655.
83. QUIK M, KULAK JM: Nicotine and nicotinic receptors; relevance to Parkinson's disease. Neurotoxicology (2002) 23(4-5):581-594.
84. GAHRING LC, MEYER EL, ROGERS SW: Nicotine-induced neuroprotection against N-methyl-D-aspartic acid or β-amyloid peptide occur through independent mechanisms distinguished by pro-inflammatory cytokines. J. Neurochem. (2003) 87(5):1125-1136.
85. WHITESIDE GT, MUNGLANI R: Cell death in the superficial dorsal horn in a model of neuropathic pain. J. Neurosci. Res. (2001) 64(2):168-173.
86. RAVIKUMAR R, FLORA G, GEDDES JW, HENNIG B, TOBOREK M: Nicotine attenuates oxidative stress, activation of redox-regulated transcription factors and induction of proinflammatory genes in compressive spinal cord trauma. Brain Res. Mol. Brain Res. (2004) 124(2):188-198.
87. RAVIKUMAR R, FUGACCIA I, SCHEFF SW et al.: Nicotine attenuates morphological deficits in a contusion model of spinal cord injury. J. Neurotrauma (2005) 22(2):240-251.