PAIN
Volume 90, Issue 3 , Pages 217-226 , 15 February 2001

The effects of GABAB agonists and gabapentin on mechanical hyperalgesia in models of neuropathic and inflammatory pain in the rat

Received 27 April 2000 ,Revised 27 July 2000 ,Accepted 9 August 2000.

References 

  1. Abdi S, Lee DH, Chung JM. The anti-allodynic effects of amitryptiline, gabapentin and lidocaine in a rat model of neuropathic pain. Anesth Analg. 1999;87:1360–1366
  2. Aran S, Hammond DL. Antagonism of baclofen-induced antinociception by intrathecal administration of phaclofen or 2-hydroxysaclofen but not d-aminovaleric acid in the rat. J Pharmacol Exp Ther. 1991;257:360–368
  3. Backonja M, Beydoun A, Edwards KR, Schwartz SL, Fonseca V, Hes M, et al. Gabapentin for the symptomatic treatment of painful neuropathy in patients with diabetes mellitus. J Am Med Assoc. 1998;280:1831–1836
  4. Barber RP, Vaughn J, Saito K, McLaughlin BJ, Roberts E. GABAergic terminals are presynaptic to primary afferent terminals in the substantia gelatinosa of the rat spinal cord. Brain Res. 1978;141:35–55
  5. Bowery NG, Hudson AL, Price GW. GABAA and GABAB receptor site distribution in the rat central nervous system. Neuroscience. 1987;20:365–383
  6. Carlton SM, Zhou S. Attenuation of formalin-induced nociceptive behaviours following local peripheral injection of gabapentin. Pain. 1998;76:201–207
  7. Castro-Lopez JM, Tavares I, Tolle TR, Coito A, Coimbra A. Increase in GABAergic cells and GABA levels in the spinal cord in unilateral inflammation of the hindlimb in the rat. Eur J Neurosci. 1992;4:296–301
  8. Castro-Lopez JM, Tavares I, Coimbra A. GABA decreases in the spinal cord dorsal horn after peripheral neurectomy. Brain Res. 1993;620:287–291
  9. Castro-Lopez JM, Malcangio M, Bowery NG. Complex changes of GABAA and GABAB receptor binding in the spinal cord dorsal horn following peripheral inflammation or neurectomy. Brain Res. 1995;679:289–297
  10. Chapman V, Suzuku R, Chamarette HLC, Rygh LJ, Dickenson AH. Effects of systemic carbamazepine and gabapentin on spinal neuronal responses in spinal nerve ligated rats. Pain. 1998;75:261–272
  11. Curtis DR, Lacey G. GABA-B receptor-mediated spinal inhibition. NeuroReport. 1994;5:540–542
  12. Dickenson AH, Brewer CM, Hayes NA. Effects of topical baclofen on C fibre-evoked neuronal activity in the dorsal horn. Neuroscience. 1985;14:557–562
  13. Dubner R, Ruda MA. Activity-dependent neuronal plasticity following tissue injury and inflammation. Trends Neurosci. 1992;15:96–103
  14. Field MJ, McClearly S, Hughes J, Singh L. Gabapentin and pregabalin, but not morphine and amytriptiline, block both static and dynamic components of mechanical allodynia induced by streptozotocin in the rat. Pain. 1999;80:391–398
  15. Froestl W, Mickel SJ, Hall RG, von Sprecher G, Strub D, Baumann PA, et al. Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995;38:3297–3312
  16. Fromm GH. Baclofen as an adjuvant analgesic. J Pain Sympt Manage. 1994;9:500–509
  17. Fromm GH, Terrence CF, Chattha AS. Baclofen in the treatment of trigeminal neuralgia: double-blind study and long-term follow-up. Ann Neurol. 1984;15:240–244
  18. Gee NS, Brown JP, Dissananyake VUK, Offord J, Thurlow R, Woodruff GN. The novel anticonvulsant drug gabapentin (Neurontin) binds to the α2δ subunit of a calcium channel. J Biol Chem. 1996;271:5768–5776
  19. Hammond DL, Drower EJ. Effects of intrathecally administered THIP, baclofen and muscimol on nociceptive threshold. Eur J Pharmacol. 1984;103:121–125
  20. Hunter JC, Gogas KR, Hedley LR, Jacobson LO, Kassotakis L, Thompson J, et al. The effect of novel anti-epileptic drugs in rat experimental models of acute and chronic pain. Eur J Pharmacol. 1997;324:153–160
  21. Hwang JH, Yaksh TL. The effect of spinal GABA receptor agonists on tactile allodynia in a surgically-induced neuropathic pain model in the rat. Pain. 1997;70:15–22
  22. Kangra I, Jiang M, Randic M. Actions of (−)baclofen on rat dorsal horn neurons. Brain Res. 1991;562:265–275
  23. Kocsis JD, Honmou O. Gabapentin increases GABA-induced depolarisation in rat neonatal optic nerve. Neurosci Lett. 1994;169:181–190
  24. Laird JMA, Bennett GJ. Dorsal root potentials and afferent input to the spinal cord in rats with an experimental peripheral neuropathy. Brain Res. 1992;584:181–190
  25. Magoul R, Onteniente B, Geffard M, Calas A. Anatomical distribution and ultrastructural organization of the GABAergic system in the rat spinal cord: an immunohistochemical study using anti-GABA antibodies. Neuroscience. 1987;20:1001–1009
  26. Malcangio M, Bowery NG. GABAB receptor-mediated inhibition of forskolin-stimulated cyclic AMP accumulation in rat spinal cord. Neurosci Lett. 1993;158:189–192
  27. Malcangio M, Bowery NG. GABA and its receptors in the spinal cord. Trends Pharmacol Sci. 1996;17:457–462
  28. Malcangio M, Ghelardini C, Giotti A, Malmberg-Aiello P, Bartolini A. CGP 35348, a new GABAB antagonist, prevents antinociception and muscle relaxant effect induced by baclofen. Br J Pharmacol. 1991;103:1303–1308
  29. Mellick GA, Mellick B. Gabapentin in the management of reflex sympathetic dystrophy. J Pain Sympt Manage. 1995;10:265–266
  30. Pan HL, Eisenach JC, Chen SR. Gabapentin suppresses ectopic discharges and reverses allodynia in neuropathic rats. J Pharmacol Exp Ther. 1999;288:1026–1030
  31. Penn RD, Kroin JS. Continuous intrathecal baclofen for severe spasticity. Lancet. 1985;ii:125–127
  32. Price GW, Wilkin GP, Turnbull MJ, Bowery NG. Are baclofen-sensitive GABAB receptors present on primary afferent terminals of the spinal cord?. Nature. 1984;307:376–380
  33. Price GW, Kelly JS, Bowery NG. The location of GABAB receptor binding sites in mammalian spinal cord. Synapse. 1987;1:530–538
  34. Rowbotham M, Harden N, Stacey B. Gabapentin for the treatment of postherpetic neuralgia. J Am Med Assoc. 1998;280:1837–1842
  35. Sawynok J. GABAergic mechanism of analgesia: an update. Pharmacol Biochem Behav. 1987;26:463–474
  36. Sawynok K, La Bella FS. On the involvement of GABA in the analgesia produced by baclofen, muscimol and morphine. Neuropharmacology. 1982;21:397–403
  37. Seabrook GR, Howson W, Lacey MG. Electrophysiological characterization of potent agonists and antagonists at pre- and postsynaptic GABAB receptors on neurones in rat brain slices. Br J Pharmacol. 1990;101:949–957
  38. Seltzer Z, Dubner R, Shir Y. A novel behavioural model of neuropathic pain disorders produced in rats by partial sciatic nerve injury. Pain. 1990;43:205–218
  39. Shimoyama N, Shimoyama KM, Davis AM, Inturrisi CE, Elliot KJ. Spinal gabapentin is antinociceptive in the rat formalin test. Neurosci Lett. 1997;222:65–67
  40. Sivilotti L, Woolf CJ. The contribution of GABAA and glycine receptors to central sensitization: disinhibition and touch-evoked allodynia in the spinal cord. J Neurophysiol. 1994;72:169–179
  41. Smith GD, Harrison SM, Birch PJ, Elliott PJ, Malcangio M, Bowery NG. Increased sensitivity to the antinociceptive activity of ± baclofen in an animal model of chronic neuropathic, but not chronic inflammatory hyperalgesia. Neuropharmacology. 1994;33:1103–1108
  42. Sugimoto T, Bennett GJ, Kajander KC. Transynaptic degeneration in the superficial dorsal horn after sciatic nerve injury: effects of chronic constriction injury, transection, and strychnine. Pain. 1990;42:205–213
  43. Teoh H, Malcango M, Bowery NG. GABA, glutamate and substance P-like immunoreactivity release: effects of novel GABAB antagonists. Br J Pharmacol. 1996;118:1153–1160
  44. Thompson SWN, Urban L, Dray A. Contribution of NK1 and NK2 receptor activation to high threshold afferent fibre evoked ventral root responses in the rat spinal cord in vitro. Brain Res. 1993;625:100–108
  45. Todd AJ, Lockhead ?. Gaba-like immunoreactivity in type 1 glomueruli of rat substantia gelatinosa. Brain Res. 1990;514:171–174
  46. Todd AJ, McKenzie J. GABA-immunoreactive neurons in the dorsal horn of the rat spinal cord. Neuroscience. 1989;31:799–806
  47. Xiao WH, Bennett GJ. Gabapentin relieves abnormal pains in a rat model of painful peripheral neuropathy. Soc Neurosci Abstr. 1995;21:897
  48. Yaksh TL. Behavioural and autonomic correlates of the tactile evoked allodynia produced by spinal glycine inhibition: effect of modulatory receptor systems and excitatory amino acid antagonists. Pain. 1989;37:111–123
  49. Yoon MH, Yaksh TL. The effect of intrathecal gabapentin on pain behaviour and hemodynamics in the formalin test in the rat. Anesth Anal. 1999;89:434–439
  50. Young RR, Delwaide PJ. Drug therapy: spasticity. N Engl J Med. 1981;304:28–33

PII: S0304-3959(00)00404-8

PAIN
Volume 90, Issue 3 , Pages 217-226 , 15 February 2001