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Review

The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control

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Pages 1819-1830 | Published online: 24 Feb 2005

Bibliography

  • REISINE T, PASTERNAK G: Opioid analgesics and antagonists. In: Goodman & Gilman 's The Pharmacological Basis of Therapeutics, 9th Edition. JG Hardman et al. (Ed.) . McGraw-Hill, New York, USA. (1996):521–555.
  • INSEL PA: Analgesic-antipyretic and antiinflammatory agents and drugs employed in the treatment of gout, In: Goodman & Gilman 's The Pharmacological Basis of Therapeutics, 9th Edition, JG Hardman et al. (Eds.) McGraw-Hill, New York, USA. (1996):617–657.
  • OLLAT H, CESARO P: Pharmacology of neuropathic pain. OM. Neuropharmacol (1995) 18:391–404.
  • MARNETT LJ, KALGUTKAR AS: Cyclooxygenase 2 inhibitors: discovery, selectivity and the future. Trends Pharmacol. Sci. (1999) 20:465–469.
  • WILLIAMS M, KOWALUK EA, ARNERIC SP: Emerging molecular approaches to pain therapy. I Med. Chem. (1999) 42:1481–1500.
  • ••A review of novel therapeutic approachesto pain relief.
  • DECKER MW, MEYER MD: Therapeutic potential of neuronal nicotinic acetylcholine receptor agonists as novel analgesics. Biochem. Pharmacol (1999) 58: 917–923.
  • •A review of the potential of nAChR agonists as analgesics.
  • FLORES CM: The promise and pitfalls of a nicotinic cholinergic approach to pain management. Pain (2000) 88:1–6.
  • •A review of the potential of nAChR agonists as analgesics.
  • GOTTI C, FORNASARI D, CLEMENTI F: Human neuronal nicotinic receptors. Prog. Neurobiol (1997) 53:199–237.
  • CHANGEUX J-P: The nicotinic acetylcholine receptor: an allosteric protein prototype of ligand-gated ion channels. Trends Pharmacol Sci. (1990) 11:485–491.
  • BOYD RT: The molecular biology of neuronal nicotinic acetylcholine receptors. Critical Rev Toxicol. (1997) 27:299–318.
  • CHEN DN, PATRICK JW: The alpha-bungarotoxin-binding nicotinic acetylcholine-receptor from rat-brain contains only the alpha-7 subunit. j Biol. Chem. (1997) 272:24024–24029.
  • DRISDEL RC, GREEN WN: Neuronal alpha-bungarotoxin receptors are alpha 7 subunit homomers. j Neurosci. (2000) 20:133–139.
  • FLORES CM, ROGERS SW, PABREZA LA, WOLFE BB, KELLAR KJ: A subtype of nicotinic cholinergic receptor in rat brain is composed of a4 and 32 subunits and is upregulated by chronic nicotine treatment. Pharmacol (1992) 41:31–37.
  • FLORES CM, DECAMP RIVI, KILO S, ROGERS SW, HARGREAVES KM: Neuronal nicotinic receptor expression in sensory neurons of the rat trigeminal ganglion: Demonstration of a334, a novel subtype in the mammalian nervous system. Neurosci. (1996) 16:7892–7901.
  • ••Demonstrates that both a4[32 and a34-containing nAChRs exist in the trigeminal ganglion.
  • LIU L, CHANG CQ, RAO YQ, SIMON SA: Neuronal nicotinic acetylcholine receptors in rat trigeminal Ganglia. Brain Res. (1998) 809:238–245.
  • FLORES CM, HARGREAVES KM: Neuronal nicotinic receptors: New targets in the treatment of pain, In: Neuronal Nicotinic Receptors: Pharmacology and Therapeutic Opportunities. SP Arneric, JD Brioni, (Eds.) Wiley-Liss, New York, USA. (1998):359–378.
  • DECKER MW, ARNERIC SP: Nicotinic acetylcholine receptor-targeted compounds: A summary of the development pipeline and therapeutic potential, In: Neuronal Nicotinic Receptors: Pharmacology, and Therapeutic Opportunities, SP Arneric and JD Brioni (Eds.) Wiley-Liss, New York, USA. (1998):395–411.
  • DAVIS L, POLLOCK LJ, STONE T: Visceral pain. Surg. Cyrrecol Obstet. (1932) 55:418–426.
  • DALY JW, GARRAFFO HM, SPANDE TF, DECKER MW SULLIVAN JP, WILLIAMS M: Alkaloids from frog skin: the discovery of epibatidine and the potential for developing novel non-opioid analgesics. Natural Product Reports (2000) 17:131–135.
  • ••In this paper, Daly describes his discoveryof epibatidine.
  • SULLIVAN JP, DECKER MW, BRIONI JD et al.: (±)-Epibatidine elicits a diversity of in vitro and in vivo effects mediated by nicotinic acetylcholine receptors. Pharmacol Exp. Ther. (1994) 271:624–631.
  • SULLIVAN JP, BRIGGS CA, DONNELLY-ROBERTS D et al: (±)- Epibatidine can differentially evoke responses mediated by putative subtypes of nicotinic acetylcholine receptors (nAChRs). Med. Chem. Res. (1994) 4:502–516.
  • BADIO B, DALY JW: Epibatidine, a potent analgetic and nicotinic agonist. Pharmacol.(1994) 45:563–569.
  • LEMBECK F: Epibatidine: high potency and broad spectrum activity on neuronal and neruomuscular nicotinic acetylcholine receptors. Naurryn-Schmiedebergs Arch. Pharmacol (1999) 359:378–385.
  • TRAYNOR JR: Epibatidine and pain. Br. Arraesth. (1998) 81:69–76.
  • •An excellent review of the analgesic effects of epibatidine.
  • CURZON E NIKKEL AL, BANNON AW, ARNERIC SP, DECKER MW: Differences between the antinociceptive effects of the cholinergic channel activators A-85380 and (+/-)-epibatidine in rats. Pharmacol Exp. Ther. (1998) 287:847–853.
  • •Provides a direct comparison of the antinociceptive and locomotor effects of A-85380 and epibatidine and examines the role of the nucleus raphe magnus in these effects.
  • KESINGLAND AC, GENTRY CT, PANESAR MS et al.: Analgesic profile of the nicotinic acetylcholine receptor agonists, (-0-epibatidine and ABT-594 in models of persistent inflammatory and neuropathic pain. Pain (2000) 86:113–118.
  • LAWAND NB, LU Y, WESTLUND KN: Nicotinic cholinergic receptors: potential targets for inflammatory pain relief. Pain (1999) 80:291–299.
  • GILBERT SD, CLARK TM, FLORES CM: Antihyperalgesic activity of epibatidine in the formalin model of facial pain. Pain (2001) 89:159–165.
  • SULLIVAN JP, DONNELLY-ROBERTS D, BRIGGS CA et al: A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. Neuropharmacology (1996) 35:725–734.
  • BANNON AW, DECKER MW HOLLADAY MW et al.: Broad spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors. Science (1998) 279:77–81.
  • ••First description of the novel nAChRanalgesic ABT-594.
  • DONNELLY-ROBERTS DL,
  • PUTTFARCKEN PS, KUNTZWEILER TA et al.: ABT-594 [(R) 5 (2 azetidinylmethoxy)-2-chloropyridinel - a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors - I - in vitro characterization. j PharmacoL Exp. Ther. (1998) 285:777–786.
  • HOLLADAY MW, BAT H, LI YH et al.: Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent - effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice. Bioorganic Med. Chem. Lett. (1998) 8:2797–2802.
  • HOLLADAY MW, WASICAK JT, LIN NH et al.: Identification and initial structure-activity relationships of (R) 5 (2 azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via reuronal ricotinic acetylcholine receptors. I Med. Chem. (1998) 41:407–412.
  • HOLLADAY MW, DECKER MW: Discovery of ABT-594 and related neuronal nicotinic acetylcholine receptor modulators as analgesic agents: Medicinal chemistry and biology. Adv. Med. Chem. (2000) 5:85–113.
  • MEYER MD, DECKER MW, RUETER LE et al.: The identification of novel structural compound classes exhibiting high affinity for neuronal nicotinic acetylcholine receptors and analgesic efficacy in preclinical models of pain. Eur. Pharmacol (2000) 393:171–177.
  • BANNON AW, DECKER MW, KIM DJB, CAMPBELL JE, ARNERIC SP: ABT-594, a novel cholinergic channel modulator, is efficacious in nerve ligation and diabetic neuropathy models of neuropathic pain. Brain Res. (1998) 801:158–163.
  • DECKER MW, BANNON AW, BUCKLEY MJ et al.: Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in mice. Eur. j PharmacoL (1998) 346:23–33.
  • BANNON AW, DECKER MW, CURZON P et al.: ABT-594 [(R) 5 (2 azetidinylmethoxy)-2-chloropyridinel - a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors. II. in vivo characterization. Pharmacol Exp. Ther. (1998) 285:787–794.
  • BOYCE S, WEBB JK, SHEPHEARD SL, RUSSELL MGN, HILL RG, RUPNIAK NMJ: Analgesic and toxic effects of ABT-594 resemble epibatidine and nicotine in rats. Pain (2000) 85:443–450.
  • BARLOCCO D, CIGNARELLA G, TONDI D etal.: Mono- and disubstituted-3, 8-diazabicyclo [3.2.11 octane derivatives as analgesics structurally related to epibatidine - synthesis, activity, and modeling. I Med. Chem. (1998) 41:674–681.
  • GHELARDINI C, GALEOTTI N, BARLOCCO D, BARTOLINI A: Antinociceptive profile of the new nicotinic agonist DBO-83. Drug Dev. Res. (1997) 40:251–258.
  • VERNIER JM, HOLSENBACK H, COSFORD NDP et al.: Conformationally restricted analogs of nicotine and anabasine. Bioorg. Med. Chem. Lett. (1998) 8:2173–2178.
  • •Description of SIB-1663.
  • GLASSCO W, SUCHOCKI J, GEORGE C, MARTIN BR, MAY EL: Synthesis, optical resolution, absolute configuration and preliminary pharmacology of (-0 and (-)-cis-2,3,3a,4,5,9b-hexahydro-1-methy1-11--/-pyrrolo[3,2-1disoquinoline, a structural analog of nicotine. I Med. Chem. (1993) 36:3381–3385.
  • BENCHERIF M, LOVETTE ME, FOWLER KW et al.: RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization. I PharmacoL Exp. Ther. (1996) 279:1413–1421.
  • DAMAJ MI, GLASSCO W, ACETO MD, MARTIN BR: Antinociceptive and pharmacological effects of metanicotine, a selective nicotinic agonist. I PharmacoL Exp. Ther. (1999) 291:390–398.
  • •Provides a thorough evaluation of the antinociceptive effects of RJR-2403 (metanicotine).
  • BRIGGS CA, ANDERSON DJ, BRIONI JD et al.: Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. PharmacoL Biochem. Behav. (1997) 57: 231–241.
  • MEYER EM, TAY ET, PAPKE RL, MEYERS C, HUANG GL, DE FIEBRE CM: 3- [2,4-dimethoxybenzylidene] anabaseine (DMX13) selectively activates rat a7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner. Brain Res. (1997) 768:49–56.
  • DECKER M, BRIONI J, BANNON A, ARNERIC S: Diversity of neuronal nicotinic acetylcholine receptors: lessons from behavior and implications for CNS therapeutics. Life Sci. (1995) 56:545–570.
  • SULLIVAN JP, DONNELLY-ROBERTS D, BRIGGS CA et al.: ABT-089 [2-methyl- 3(2- (S)-pyrrolidinylmethoxy)pyridine] .1. a potent and selective cholinergic channel modulator with neuroprotective properties. PharmacoL Esp. Ther. (1997) 283:235–246.
  • BRIONI JD, KIM DJB, O'NEILL A, BRODIE MS, DECKER MW, ARNERIC SP: ABT-089 [2-methyl-3 (2-(S)-pyrrolidinylmethoxApyridine dihydrochloridel: Discriminative stimulus properties and electrophysiological actions. Drug Dev. Res. (1997) 40:259–166.
  • NANRI M, YAMAMOTO J, MIYAKE H, WATANABE H: Protective effect of GTS-21, a novel nicotinic receptor agonist, on delayed neuronal death induced by ischemia in gerbils. Japanese I PharmacoL (1998) 76:23–29.
  • BANNON AW, GUNTHER KL, DECKER MW: Is epibatidine really analgesic? Dissociation of the activity, temperature, and analgesic effects of (-4-epibatidine. PharmacoL Biochem. Behav. (1995) 51:693–698.
  • DAMAJ MI, FEIYIN M, DUKAT M, GLASSCO W GLENNON RA, MARTIN BR: Antinociceptive responses to nicotinic acetylcholine receptor ligands after systemic and intrathecal administration in mice. PharmacoL Esp. Ther. (1998) 284:1058–1065.
  • ••Provides a thorough evaluation of theeffects of a variety of nAChR agonists after spinal or systemic administration. Also demonstrates that the nAChR agonists differ in their sensitivities to mecamylamine and DHBE.
  • RAO TS, CORREA LD, REID RT, LLOYD GK: Evaluation of anti-nociceptive effects of neuronal nicotinic acetylcholine receptor (nAChR) ligands in the rat tail-flick assay. Neuropharmacology (1996) 35:393–405.
  • DAMAJ MI, MEYER EM, MARTIN BR: The antinociceptive effects of alpha 7 nicotinic agonists in an acute pain model. Neuropharmacology (2000) 39:2785–2791.
  • MARUBIO LM, ARROYO-JIMENEZ MD, CORDERO-ERAUSQUIN M et al.: Reduced antinociception in mice lacking neuronal nicotinic receptor subunits. Nature (1999) 398:805–810.
  • ••Demonstrates the importance of a4- and[32-containing nAChRs in nicotine-induced antinociception using knockout mice.
  • BITNER RS, NIKKEL AL, CURZON P etal.: Reduced nicotinic receptor-mediated antinociception following in vivo antisense knock-down in rat. Brain Res. (2000) 871:66–74.
  • CAGGIULA AR, EPSTEIN LH, PERKINS KA, SAYLOR S: Different methods of assessing nicotine-induced antinociception may engage different neural mechanisms. Psychopharmacology (1995) 122:301–306.
  • IWAMOTO ET: Characterization of theantinociception induced by nicotine in the pedunculopontine tegmental nucleus and the nucleus raphe magnus. j Pharmacol Exp. Ther. (1990) 257:120–133.
  • BITNER RS, NIKKEL AL, CURZON P, ARNERIC SP, BANNON AW, DECKER MW: Role of the nucleus raphe magnus in antinociception produced by ABT-594 - Immediate early gene responses possibly linked to neuronal nicotinic acetylcholine receptors on serotonergic neurons. Neurosci. (1998) 18:5426–5432.
  • •Describes the co-localisation of the a4 subunit of the nAChR and serotonin.
  • NUSEIR K, HEIDENREICH BA, PROUDFIT HK: The antinociception produced by microinjection of a cholinergic agonist in the ventromedial medulla is mediated by noradrenergic neurons in the Al catecholamine cell group. Brain Res. (1999) 822:1–7.
  • PAN HL, CHEN SR, EISENACH JC: Intrathecal clonidine alleviates allodynia in neuropathic rats - Interaction with spinal muscarinic and nicotinic receptors. Anesthesiology (1999) 90:509–514.
  • DECKER MW CURZON E HOLLADAY MW et al: The role of neuronal nicotinic acetylcholine receptors in antinociception: Effects of ABT-594. Physic] (Paris) (1998) 92:221–224.
  • ROGERS DT, IWAMOTO ET: Multiple spinal mediators in parenteral nicotine-induced antinociception. j Pharmacol Exp. Ther. (1993) 267:341–349.
  • RUETER LE, MEYER MD, DECKER MW: Spinal mechanisms underlying A-85380-induced effects on acute thermal pain. Brain Res. (2000) 872:93–101.
  • HOGLUND AU, HAMILTON C, LINDBLOM L: Effects of microdialyzed oxotremorine, carbachol, epibatidine, and scopolamine on intraspinal release of acetylcholine in the rat. j Pharmacol Exp. Ther. (2000) 295:100–104.
  • KHAN IM, YAKSH TL, TAYLOR P: Epibatidine binding sites and activity in the spinal cord. Brain Res. (1997) 753:269–282.
  • KHAN IM, BUERKLE H, TAYLOR E YAKSH TL: Nociceptive and antinociceptive responses to intrathecally administered nicotinic agonists. Neuropharmacology (1998) 37:1515–1525.
  • ••Identifies a biphasic effect of it. epibatidineand suggests that pronociceptive and antinociceptive effects are mediated by different nAChR subtypes.
  • KHAN IM, STANISLAUS S, ZHANG L, TAYLOR E YAKSH TL: A-85380 and epibatidine each interact with disparate spinal nicotinic receptor subtypes to achieve analgesia and nociception. j Pharmacol Exp. Ther. (2001) 297:230–239.
  • CHIARI A, EISENACH JC: Sex differences in cholinergic analgesia in normal rats. Anesthesiology (1998) 89:A1079–A1079.
  • LAVAND'HOMME PM, EISENACH JC: Sex differences in cholinergic analgesia II: Differing mechanisms in two models of allodynia. Anesthesiology (1999) 91:1455–1461.
  • CHIARI A, TOBIN JR, PAN H-LMD, HOOD DD, EISENACH JC: Sex differences in cholinergic analgesia I: A supplemental nicotinic mechanism in normal females. Anesthesiology (1999) 91:1447–1454.
  • WONNACOTT S: Presynaptic nicotinicACh receptors. Trends Neurosci. (1997) 20:92–98.
  • WEWERS ME, DHATT RK, SNIVELY TA, TEJWANI GA: The effect of chronic administration of nicotine on antinociception, opioid receptor binding and met-enkelphalin levels in rats. Brain Res. (1999) 822:107–113.
  • ZHU PJ, CHIAPPINELLI VA: Nicotinemodulates evoked GABAergic transmission in the brain. j Neurophysiol (1999) 82:3041–3045.
  • SALMON AM, DAMAJ MI, MARUBIO LM, EPPING-JORDAN MP, MERLO-PICH E, CHANGEUX JP: Altered neuroadaptation in opiate dependence and neurogenic inflammatory nociception in alpha CGRP-deficient mice. Nat. Neuro. (2001) 4:357–358.
  • DAMAJ MI: The involvement of spinal Ca2Vcalmodulin-protein kinase II in nicotine-induced antinociception in mice. Eur. Pharmacol (2000) 404:103–110.
  • MALIN DH, LAKE JR, CARTER VA, CUNNINGHAM JS, WILSON OB: Naloxone precipitates nicotine abstinence syndrome in the rat. Psychopharmacology (1993) 112:339–342.
  • ZARRINDAST MR, NAMI AB, FARZIN D: Nicotine potentiates morphine antinociception: a possible cholinergic mechanism. Eur. Neuropsychopharmacol (1996) 6:127–133.
  • ZARRINDAST MR, KHOSHAYAND MR, SHAFAGHI B: The development of cross-tolerance between morphine and nicotine in mice. Eur. Neuropsychopharmacol (1999) 9:227–233.
  • DAMAJ MI, CREASY KR, GROVE AD, ROSECRANS JA, MARTIN BR: Pharmacological effects of epibatidine optical enantiomers. Brain Res. (1994) 664:34–40.
  • JAMNER LD, GIRDLER SS, SHAPIRO D, JARVIK ME: Pain inhibition, nicotine, and gender. Exp. Clin. Psychopharmacol (1998) 6:96–106.
  • •An analysis of the role of gender in responses to nicotine using an experimental pain model in humans. Also provides evidence that the efficacy achieved with nicotine is comparable to that achieved with some analgesics.
  • SLADE J, HENNINGFIELD JE: Tobacco product regulation: context and issues. Food Drug Law J. (1998) 53:43–74.
  • PICKWORTH WB, BUNKER EB, HENNINGFIELD JE: Transdermal nicotine: reduction of smoking with minimal abuse liability. Psychopharmacology (1994) 115:9–14.
  • WEST R, HAJEK P, FOULDS J, NILSSON F, MAY S, MEADOWS A: A comparison of the abuse liability and dependence potential of nicotine patch, gum, spray and inhaler. Psychopharmacology (2000) 149:198–202.
  • PICCIOTTO MR, ZOLI M, RIMONDINI R etal.: Acetylcholine-receptors containing the 132 subunit are involved in the reinforcing properties of nicotine. Nature (1998) 391:173–177.
  • ••Uses p2 knockout mice to demonstratethat [32-containing nAChRs at involved in nicotine self-administration and nicotine-induced dopamine release.
  • SHOAIB M, STOLERMAN IP, KUMAR RC: Nicotine-induced place preferences following prior nicotine exposure in rats. Psychopharmacology (1994) 113:445–452.
  • MCCALLUM SE, CAGGIULA AR, BOOTH S et al.: Mecamylamine prevents tolerance but enhances whole brain epibatidine binding in response to repeated nicotine administration in rats. Psychapharmacalagy (2000) 150:1–8.
  • MCCALLUM SE, CAGGIULA AR, EPSTEIN LH, SAYLOR S, PLOSKINA T, SVED AF: Mecamylamine blocks the development of tolerance to nicotine in rats: implications for the mechanisms of tolerance. Psychapharmacalagy (1999) 141:332–338.
  • CEPEDA-BENITO A, REYNOSO J, MCDANIEL EH: Associative tolerance to nicotine analgesia in the rat: tail-flick and hot-plate tests. Exp. Clin. Psychapharmacal. (1998) 6:248–254.
  • DAMAJ MI, MARTIN BR: Tolerance to the antinociceptive effect of epibatidine after acute and chronic administration in mice. Eur. Pharmacal. (1996) 300:51–57.
  • KEST B, WILSON SG, MOGIL JS: Sex differences in supraspinal morphine analgesia are dependent on genotype. j. Pharmacal. Exp. Ther. (1999) 289:1370–1375.
  • •Compares antinociceptive response to morphine of males and females from 11 inbred mouse strains, demonstrating sex differences, strain differences, and strain by sex interactions.
  • FLORES CM, WILSON SG, MOGIL JS: Pharmacogenetic variability in neuronal nicotinic receptor-mediated antinociception. Pharmacagerietics (1999) 9: 619–625.
  • ••The antinociceptive response toepibatidine are evaluated across 8 inbred mouse strains, with strain differences in both potency and duration of action being identified.
  • CRAFT RIVI, MILHOLLAND RB: Sex differences in cocaine- and nicotine-induced antinociception in the rat. Brain Res. (1998) 809:137–140.
  • DAMAJ MI: Influence of gender and sexhormones on nicotine acute pharmacological effects in mice. j. Pharmacal. Exp. Ther. (2001) 296:132–140.
  • •Examines the effects of gender of the potency of nicotine in ICR mice and evaluates the influence of sex hormones on nicotinic effects.
  • HILL R: NKi (substance P) receptor antagonists - why are they not analgesic in humans? Trends Pharinacal. Sci. (2000) 21:244–246.

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